- Asymmetric Synthesis and Antitumor Activity of Spiro-Oxadiazole Derivatives from 1,4:3,6-Dianhydro-D-fructose
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A series of spiro-oxadiazoles were synthesized from 1,4:3,6-dianhydro-D-fructose and hydrazides via a stereo- selective two-step reaction sequence. The structures of newly synthesized compounds were established by spectral analysis. The absolute configuration of compound 2a was further confirmed by single crystal X-ray analysis. All the synthesized compounds were screened for their in vitro antitumor activity, showing that these compounds have poor inhibitory activities against A549, MGC-803 tumor cells.
- Xu, Wenke,Ge, Yongxun,Hou, Yu,Liu, Yingju,Hua, Yingchun,Han, Weiwei,Qin, Zhiyan,Liu, Fengwu
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- Pentanuclear [2.2] spirocyclic lanthanide(iii) complexes: slow magnetic relaxation of the DyIII analogue
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The reaction of LnCl3·6H2O (Ln = Dy3+, Tb3+ and Ho3+) with the multisite coordinating ligand N′-(2-hydroxy-3-(hydroxymethyl)-5-methylbenzylidene)acetohydrazide (LH3) in the presence of pivalic acid (PivH) leads to the formation of three isostructural homometallic pentanuclear complexes, [Dy5(LH)4(η1-Piv)(η2-Piv)3(μ2-η2η1Piv)2(H2O)]·Cl·9·5H2O·5MeOH (1), [Tb5(LH)4(η1-Piv)(η2-Piv)3(μ2-η2η1Piv)2(H2O)]·Cl·10.5H2O·2MeOH·2CHCl3 (2) and [Ho5(LH)4(η1-Piv)(η2-Piv)3(μ2-η2η1Piv)2(H2O)]·Cl·14.5H2O·2CHCl3 (3). 1-3 are monocationic and are comprised of four doubly deprotonated [LH]2- ligands along with six pivalate ions. These complexes possess a [2.2] spirocyclic topology formed by the fusion of two triangles of LnIII ions at a common vertex. The magneto chemical analysis reveals the presence of antiferromagnetic exchange interactions at low temperature, and the DyIII complex 1 gives an out-of-phase signal with a small curvature in alternating current (ac) magnetic susceptibility measurement. Application of a 3000 G static field during ac measurement intensifies the signals, revealing a second slow relaxation process in the DyIII analogue.
- Biswas, Sourav,Das, Sourav,Van Leusen, Jan,K?gerler, Paul,Chandrasekhar, Vadapalli
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- Facile synthesis of new 10-substituted-5H-naphtho[1,2-e][1,2,4]triazolo[3,4-b][1,3,4]thiadiazin-5-ones
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The reaction of 2-bromo-1,4-naphthoquinone with 4-amino-5-aryl-4H-1,2,4-triazole-3-thiols in ethanol at 50 °C gave the corresponding 2-[(4-amino-5-aryl-4H-1,2,4-triazol-3-yl)thio]naphthalene-1,4-diones. Their treatment with EtOH/HCl under reflux conditions produced 10-substituted-5H-naphtho[1,2-e][1,2,4]triazolo[3,4-b][1,3,4]thiadiazin-5-ones through intramolecular cyclization.
- Khalafy, Jabbar,Mohammadlou, Mahsa,Mahmoody, Miri,Salami, Fatemeh,Poursattar Marjani, Ahmad
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- Synthesis, crystal structure and biological activity of 4-Cyclopropyl-3-[(3-fluorobenzyl)thio]-5-methyl-4H-1,2,4-triazole Monohydrate
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The compound 4-cyclopropyl-3-[(3-fluorobenzyl)thio]-5-methyl-4H-1,2,4- triazole monohydrate (C13H14N3SF.H 2O) were synthesized and recrystallized from ethanol. The compound was characterized by 1H NMR, elemental analyses and X-ray diffraction. The compound crystallized in the orthorhombic space group Pbca with a = 10.513(2), b = 8.4646(17), c = 30.965(6) ?, α = 90, β= 90, γ =90°, V = 2755.6(10) ?3, Z = 8 and R = 0.0510 for 2542 observed reflections with I> 2σ(I). X-ray analysis reveals that not only intermolecular O-H?N interactions, but also C-H?? stacking interactions exist in the adjacent molecules. The biological activities results showed that it exhibited significant herbicidal activity against Brassica napus.
- Ke, Wei,Sun, Na-Bo,Wu, Hong-Ke
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- Consecutive hydrazino-Ugi-azide reactions: Synthesis of acylhydrazines bearing 1,5-disubstituted tetrazoles
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Isocyanide-based multicomponent reactions (IMCRs) allow the construction of relatively complex molecules through a one-pot synthesis. The combination of IMCRs in a consecutive or sequential fashion further extends the complexity of the molecules obtained. Herein, we report the efficient application of this approach to the synthesis of acylhydrazines bearing 1,5-disubstituted tetrazoles. Our strategy was accomplished in only three steps: first, a one-pot hydrazino-Ugi-azide four-component reaction; second a hydrazinolysis and finally an additional hydrazino-Ugi-azide reaction. This sequence provides the title compounds in moderate to excellent yields. The products synthesized herein contain functional groups within their structures that can be easily modified to obtain new acylhydrazino 1,5-disubstituted tetrazoles.
- De Fátima Barreto, Angélica S.,Dos Santos, Veronica Alves,Zandrade, Carlos Kleber
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- Novel route for the transformation of a pyrimidine ring using hydrazides
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It has been shown from X-ray structural analytical data that the reaction of 2-ethoxycarbonylmethyl-1,4,6-trimethylpyrimidinium iodide with carboxylic acid hydrazides gives pyrazolo[1,5-a]pyrimidine derivatives and not the isomeric triazolo[4,3-a]pyridines previously reported. This novel and previously unreported rearrangement of 1,2-dialkylpyrimidinium salts occurs via recyclization of the pyrimidine ring with inclusion of a fragment of the nucleophilic reagent into the transformation product. 2006 Springer Science+Business Media, Inc.
- Danagulyan,Tadevosyan,Tamazyan,Panosyan
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- Acid hydrolysis of 1,6-dihydro-4-amino-3-methyl-6-phenyl-1,2,4-triazin- 5(4H)-one (1,6-dihydrometamitron)
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Metamitron (1) does not undergo hydrolysis at pH 1-8 and up to 5 M H2SO4. The product of its two-electron reduction, 1,6-dihydrometamitron (2), on the other hand, undergoes at pH 22+) predominating in strongly acidic media undergoes hydrolysis slower than the species bearing one less proton (AH+]. The latter most reactive species is present in highest concentration in solutions of pH between 0 and 2. This species is protonated on the 2,3- azomethine bond and yields as final products 2-hydrazino-2-phenylacetic acid (4) and a cethydrazide (5). Kinetic, polarographic, and spectrophotometric measurements indicated for the first dissociation an average value pK(a) = - 0.8, for the second pK(a) = 0.95. These observations together with the easy reduction of the 1,6-bond in metamitron (1) indicate that in nature the cleavage of metamitron may be preceded by its reduction to 1,6- dihydrometamitron (2), which is then hydrolyzed. Thus, anaerobic, reductive conditions are likely preferable for the total microbial degradation of metamitron.
- Ludvik,Jirkovsky,Urban,Zuman
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- Iminoboronate Formation Leads to Fast and Reversible Conjugation Chemistry of α-Nucleophiles at Neutral pH
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Bioorthogonal reactions that are fast and reversible under physiological conditions are in high demand for biological applications. Herein, it is shown that an ortho boronic acid substituent makes aryl ketones rapidly conjugate with α-nucleophiles at neutral pH. Specifically, 2-acetylphenylboronic acid and derivatives were found to conjugate with phenylhydrazine with rate constants of 102 to 103M-1s-1, comparable to the fastest bioorthogonal conjugations known to date. 11BNMR analysis revealed the varied extent of iminoboronate formation of the conjugates, in which the imine nitrogen forms a dative bond with boron. The iminoboronate formation activates the imines for hydrolysis and exchange, rendering these oxime/hydrazone conjugations reversible and dynamic under physiological conditions. The fast and dynamic nature of the iminoboronate chemistry should find wide applications in biology.
- Bandyopadhyay, Anupam,Gao, Jianmin
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- Catalytic conversion of glycerol to allyl alcohol; Effect of a sacrificial reductant on the product yield
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A continuous process for the conversion of glycerol to allyl alcohol, where ammonia or organic acids are added to the feed as sacrificial reductants, was investigated. Significant enhancement on the rate of formation and yield of the allyl alcohol is observed with some of the reducing agents examined over an alumina-supported iron catalyst. Optimising the molar ratio of the reductant relative to feed glycerol results in an increase in the yield of allyl alcohol from 9% (in the absence of additives) to 11.3% with ammonia, 15.1% with ammonium hydroxide, 17.8% with oxalic acid and 19.5% with formic acid. Moreover, the addition of other organic acids, which are produced in a typical glycerol conversion experiment, was studied. However, acetic and propanoic acids had little effect on the rate of formation of allyl alcohol. Analysis of the product distribution in the liquid and gas phases when oxalic and formic acids were added suggests a two-step process for the formation of allyl alcohol under the operating conditions of the reaction; the initial step involves the dehydration of glycerol while the second comprises the reduction of the species produced in step one. the Partner Organisations 2014.
- Sanchez, Gizelle,Friggieri, Jarrod,Adesina, Adesoji A.,Dlugogorski, Bogdan Z.,Kennedy, Eric M.,Stockenhuber, Michael
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- Dual signaling of hydrazine by selective deprotection of dichlorofluorescein and resorufin acetates
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The highly selective chemosignaling behaviors for hydrazine by a reaction-based probe of dichlorofluorescein and resorufin acetates were investigated. Hydrazinolysis of latent dichlorofluorescein and resorufin acetate fluorochromes caused prominent chromogenic and fluorescent turn-on type signals. The probes selectively detected hydrazine in the presence of commonly encountered metal ions and anions as background. Dichlorofluorescein and resorufin acetates selectively detected hydrazine with detection limits of 9.0 × 10-8 M and 8.2 × 10-7 M, respectively. Furthermore, hydrazine was selectively detected over other closely related compounds, such as hydroxylamine, ethylenediamine, and ammonia. As a possible application of the acetate probes, hydrazine signaling in tap water was tested. The Royal Society of Chemistry 2013.
- Choi, Myung Gil,Moon, Jung Ok,Bae, Jihee,Lee, Jung Woo,Chang, Suk-Kyu
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- Synthesis and in vitro leishmanicidal activity of some hydrazides and their analogues
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Twenty-one hydrazides were synthesized by treating different esters with hydrazine hydrate. Substituted hydrazides were obtained by treating hydrazides with alkyl/aryl/acyl halides. Some of these compounds exhibit potential in vitro leishmanicidal activity. The structures of all the synthesized compounds were confirmed by spectroscopic analysis.
- Khan, Khalid Mohammad,Rasheed, Maimona,Ullah, Zia,Hayat, Safdar,Kaukab, Farhana,Choudhary, M. Iqbal,Ur-Rahman, Atta,Perveen, Shahnaz
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- An efficient CO2 fixation reaction with epoxides catalysed by: In situ formed blue vanadium catalyst from dioxovanadium(+5) complex: Moisture enhanced and atmospheric oxygen retarded catalytic activity
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Two new dioxovanadium(+5) complexes, one anionic and other neutral, have been synthesized and characterized by X-ray crystallography in this work. While doing cycloaddition reaction of CO2 to epoxides, taking dioxovanadium(+5) complex as the catalyst, a blue vanadium complex was generated in situ, which was found to be the active catalyst, showing excellent catalytic activity in the presence of tetrabutylammonium bromide as the co-catalyst. The catalytic activity of the catalyst system is enhanced by moisture and, on the other hand, is retarded by atmospheric oxygen. The enhanced catalytic activity at moistened conditions shows the applicability of the catalyst for CO2 fixation from wet flue gas. However, the retarded catalytic activity caused by atmospheric oxygen is important from the mechanistic point of view.
- Borah, Rakhimoni,Deori, Naranarayan,Brahma, Sanfaori
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- Bioisosteric approach to elucidation of binding of the acetate group of a moth sex pheromone component to its receptor
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A number of analogs of (Z)-5-decenyl acetate, a pheromone component of the turnip moth, Agrotis segetum, in which the acetate group has been replaced by functional groups that may function as bioisosters, have been synthesized and tested using single-cell electrophysiology. The activities have been interpreted in terms of the molecular electrostatic potentials of the polar functional group as calculated by ab initio quantum mechanical calculations. It is concluded that both oxygens of the acetate group in (Z)-5-decenyl acetate contribute to the interactions between the pheromone component and its receptor. Furthermore, the results indicate that the crucial interaction between the carbonyl group and the receptor, which is most probably a hydrogen bonding interaction, takes place in a direction pointing away from the hydrocarbon chain of the pheromone component.
- Gustavsson, Anna-Lena,Tuvesson, Malena,Larsson, Mattias C.,Wenqi, Wu,Hansson, Bill S.,Liljefors, Tommy
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- Tuning the exchange dynamics of boronic acid hydrazones and oximes with pH and redox control
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Dynamic bonds continually form and dissociate at equilibrium. Carbonyl compounds with proximal boronic acids, including 2-formylphenylboronic acid (2-FPBA), have been reported to form highly dynamic covalent hydrazone and oxime bonds in physiological conditions, but strategies to tune the dynamics have not yet been reported. Here, we characterize the dynamics of 2-FPBA-derived hydrazones and oximes and account for both the rapid rate of formation (~102-103M?1s?1) and the relatively fast rate of hydrolysis (~10?4s?1) at physiological pH. We further show that these substrates undergo exchange with α-nucleophiles, which can be reversibly paused and restarted with pH control. Finally, we show that oxidation of the arylboronic acid effectively abolishes the rapid dynamics, which slows the forward reaction by more than 30?000 times and increases the hydrolytic half-life from 50 minutes to 6 months at physiological pH. These results set the stage to explore these linkages in dynamic combinatorial libraries, reversible bioconjugation, and self-healing materials.
- Han, Gun Su,Domaille, Dylan W.
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- Catalytic oxygen atom transfer promoted by tethered Mo(VI) dioxido complexes onto silica-coated magnetic nanoparticles
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The preparation of three novel active and stable magnetic nanocatalysts for the selective liquid-phase oxidation of several olefins, has been reported. The heterogeneous systems are based on the coordination of cis-MoO2 moiety onto three different SCMNP@Si-(L1-L3) magnetically active supports, functionalized with silylated acylpyrazolonate ligands L1, L2 and L3. Nanocatalysts thoroughly characterized by ATR-IR spectroscopy, TGA and ICP-MS analyses, showed excellent catalytic performances in the oxidation of conjugated or unconjugated olefins either in organic or in aqueous solvents. The good magnetic properties of these catalytic systems allow their easy recyclability, from the reaction mixture, and reuse over five runs without significant decrease in the activity, either in organic or water solvent, demonstrating their versatility and robustness.
- Colaiezzi, Roberta,Crucianelli, Marcello,Di Giuseppe, Andrea,Ferella, Francesco,Lazzarini, Andrea,Paolucci, Valentina
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- Synthesis of novel seco-acyclo-N-diazolyl-thione nucleosides analogous derived from acetic acid: characterization, complex formation with ions Pb(II), Hg(II) and antibacterial activity
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Three diazoles namely 5-methyl-1,3,4-oxadiazole -2(3H)-thione, 5-methyl-1,3,4-thiadiazol-2(3H)-thione and 4-amino-5-methyl-2H-1,2,4-triazole-3-thiol were synthesized from acetic acid or ethyl acetate. Seco-acyclo-N-nucleoside analogous was synthesized by condensation of 1,3-benzylidine-glyceryl-2-tosylate with the three diazoles. Structural proof was based upon IR, 1H-NMR, 13C-NMR spectroscopy and MS measurements. The tendency to form complex between 1,3,4-oxadiazole and 1,3,4-thiadiazoles and Pb(II) and Hg(II) ions was achieved, and their structures were assigned by observing some changes in physical properties such as, MP, coloration, Rf (TLC), IR and UV spectroscopy. Most compounds were tested in vitro against Gram-positive and Gram-negative bacteria and showed variable activity. Hg2+ complexes of oxadiazole and thiadiazole derivatives exhibited appreciable antibacterial effect at lower MIC, compatible to the reference vancomycin. Similarly, oxadiazole-nucleoside exhibited high effect on Gram-positive bacteria. Graphic abstract: [Figure not available: see fulltext.]
- Chehrouri, Manel,Othman, Adil A.
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- Design, Synthesis, and Study of the Insecticidal Activity of Novel Steroidal 1,3,4-Oxadiazoles
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A series of novel steroidal derivatives with a substituted 1,3,4-oxadiazole structure was designed and synthesized, and the target compounds were evaluated for their insecticidal activity against five aphid species. Most of the tested compounds exhibited potent insecticidal activity against Eriosoma lanigerum (Hausmann), Myzus persicae, and Aphis citricola. Compounds 20g and 24g displayed the highest activity against E. lanigerum, showing LC50 values of 27.6 and 30.4 μg/mL, respectively. Ultrastructural changes in the midgut cells of E. lanigerum were detected by transmission electron microscopy, indicating that these steroidal oxazole derivatives might exert their insecticidal activity by destroying the mitochondria and nuclear membranes in insect midgut cells. Furthermore, a field trial showed that compound 20g exhibited effects similar to those of the positive controls chlorpyrifos and thiamethoxam against E. lanigerum, reaching a control rate of 89.5% at a dose of 200 μg/mL after 21 days. We also investigated the hydrolysis and metabolism of the target compounds in E. lanigerum by assaying the activities of three insecticide-detoxifying enzymes. Compound 20g at 50 μg/mL exhibited inhibitory action on carboxylesterase similar to the known inhibitor triphenyl phosphate. The above results demonstrate the potential of these steroidal oxazole derivatives to be developed as novel pesticides.
- Bai, Hangyu,Jiang, Weiqi,Li, Qi,Li, Tian,Ma, Shichuang,Shi, Baojun,Wu, Wenjun
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p. 11572 - 11581
(2021/10/12)
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- N-Amino-1,8-Naphthalimide is a Regenerated Protecting Group for Selective Synthesis of Mono-N-Substituted Hydrazines and Hydrazides
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A new route to synthesis of various mono-N-substituted hydrazines and hydrazides by involving in a new C?N bond formation by using N-amino-1,8-naphthalimide as a regenerated precursor was invented. Aniline and phenylhydrazines are reproduced upon reacting these individually with 1,8-naphthalic anhydride followed by hydrazinolysis. The practicality and simplicity of this C?N dihalo alkanes; developed a synthon for bond formation protocol was exemplified to various hydrazines and hydrazides. N-amino-1,8-naphthalimide is suitable synthon for transformation for selective formation of mono-substituted hydrazine and hydrazide derivatives. Those are selective mono-amidation of hydrazine with acid halides; mono-N-substituted hydrazones from aldehydes; synthesis of N-aminoazacycloalkanes from acetohydrazide scaffold and inserted to hydroxy derivatives; distinct synthesis of N,N-dibenzylhydrazines and N-benzylhydrazines from benzyl halides; synthesis of N-amino-amino acids from α-halo esters. Ecofriendly reagent N-amino-1,8-naphthalimide was regenerated with good yields by the hydrazinolysis in all procedures.
- Manoj Kumar, Mesram,Venkataramana, Parikibanda,Yadagiri Swamy, Parikibanda,Chityala, Yadaiah
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supporting information
p. 17713 - 17721
(2021/11/10)
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- Macrolide compound and synthesis method, pharmaceutical composition and application of compound
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The invention discloses a macrolide compound and a synthesis method, a pharmaceutical composition and application of the compound. When the macrolide compound or the pharmaceutically acceptable salt thereof provided by the invention is used together with beta-lactam antibiotics, the effect of the beta-lactam antibiotics on inhibiting methicillin-resistant staphylococcus aureus can be obviously improved. A test result shows that the in-vitro synergistic effect is good, and the compound is a novel synergist, can relieve the drug resistance of methicillin-resistant staphylococcus aureus (MRSA) to oxacillin, and has a good market development prospect.
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Paragraph 0174-0176
(2021/07/17)
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- A Convenient FeCl3-Mediated Synthesis of 5-Trifluoromethyl-1,2,4-triazoles from Trifluoroacetimidoyl Chlorides and Hydrazides
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A low cost FeCl3-mediated cascade annulation of trifluoroacetimidoyl chlorides and hydrazides for the efficient synthesis of 5-trifluoromethyl-1,2,4-triazoles has been developed. The transformation proceeds through a cascade base-promoted intermolecular C?N bond formation and FeCl3-mediated intramolecular dehydration sequence under mild conditions. The protocol exhibits many notable features and can be readily scaled up to gram scale. (Figure presented.).
- Du, Shiying,Wang, Le-Cheng,Yang, Zuguang,Chen, Zhengkai,Wu, Xiao-Feng
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p. 5130 - 5134
(2020/10/06)
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- Fragment-based drug discovery of triazole inhibitors to block PDEδ-RAS protein-protein interaction
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Although mutated Ras protein is well recognized as an important drug target, direct targeting Ras has proven to be a daunting task. Recent studies demonstrated that Ras protein needs PDEδ to relocate to plasma membrane to execute its signaling transduction function, which provides a new avenue for modulating the Ras protein. To find small molecules antagonizing the interactions between PDEδ and Ras, here we presented a successful application of fragment-based drug discovery of PDEδ inhibitors. Under the guidance of crystal structures, we are able to quickly optimize the initial fragment into highly potent inhibitors, with more than 2000-fold improvement in binding activity, which further adds to the arsenal towards the inhibition of Ras signaling in cancer therapy.
- Chen, Danqi,Chen, Yuehong,Lian, Fulin,Chen, Liu,Li, Yanlian,Cao, Danyan,Wang, Xin,Chen, Lin,Li, Jian,Meng, Tao,Huang, Min,Geng, Meiyu,Shen, Jingkang,Zhang, Naixia,Xiong, Bing
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p. 597 - 609
(2019/01/04)
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- Continuous hydrazide preparation method
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The invention relates to a continuous hydrazide preparation method. The preparation method includes: in a micro-channel reactor or a pipeline reactor, subjecting esters, anhydrides or acyl chloride tocontinuous reaction with hydrazine or solution of hydrazine under a solvent-free condition or in a solvent to prepare a hydrazide compound. The preparation method is simple, short in technical process, less in waste gas, wastewater and industrial residues, beneficial to environmental production and suitable for industrial production. The adopted reactor is short in reaction time, high in safety and capable of realizing continuous production. The adopted reactor is high in workshop space utilization rate, and large-scale production can be realized. By adoption of the preparation method, solvent recycling can be realized, and production cost is reduced; in addition, high raw material conversion rate, high quality stability and high purity are realized.
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Paragraph 0081-0083
(2019/04/17)
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- The invention relates to a synthetic pymetrozine intermediate [...] physiologically carbonate method
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The invention discloses a method for synthesizing a pymetrozine intermediate (oxadiazole ketone) by utilizing carbonate ester. According to the method, hydrazine hydrate and an acetic acid ester are utilized as raw materials for hydrazine-ester condensation to synthesize acethydrazide; oxadiazole ketone is generated through a ring-closure reaction between acethydrazide and carbonate ester under certain conditions. Such environmental-friendly non-toxic or low-toxic dimethyl carbonate, diphenyl carbonate or dibenzyl carbonate is utilized for replacing previously common virulent phosgene, diphosgene or triphosgene as a carbonylation ring-closure reagent; under the action of catalysts, a ring-closure cyclization reaction is performed for preparation of oxadiazole ketone; virulent phosgene and a great amount of inorganic solid hazardous waste are prevented from generating during a production process, so that major hidden dangers are reduced; the method has the advantages that the process is safe and reliable, reaction conditions are mild and easy to control, after-treatment is convenient, and an environmental-friendly effect is achieved.
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Paragraph 0049-0050; 0052-0053; 0055-0056
(2019/04/14)
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- COMPOUNDS AS NUCLEAR TRANSPORT MODULATORS AND USES THEREOF
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Provided are compounds of Formula I'-III', as well as their preparation and uses, and pharmaceutical compositions comprising these compounds and their uses as nuclear transport modulators. Provided are also uses of the compounds or pharmaceutical compositions in treating or preventing certain neurological disorders and diseases as well as certain types of cancer in humans.
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Page/Page column 92
(2019/12/28)
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- Multiple Hydrogen Bonds Promoted ESIPT and AIE-active Chiral Salicylaldehyde Hydrazide
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The simpler, the better! A series of simple and highly fluorescent salicylaldehyde hydrazide molecules (41 samples) have been designed and prepared. Even though these soft materials contain a very small π-conjugated system, they can go through multiple intramolecular and intermolecular hydrogen bonds promoted excited-state intramolecular proton-transfer (ESIPT) to display strong blue, green, yellow, and orange aggregation-induced emission (AIE) with large Stokes shifts (up to 184 nm) and high fluorescence quantum yields (Ф up to 0.20). Unusual mechanochromic fluorescence enhancements are also found in some solid samples. Through coordination, hydrogen and halogen bonds, these flexible molecules can be used as Mg2+ (Ф up to 0.46) probes, universal anion (Ф up to 0.14) and unprotected amino acids (Ф up to 0.16) probes, and chiral diamine (enantiomeric selectivity and Ф up to 0.36 and 0.062, respectively) receptors. Combining their advantages of AIE and biocompatibility, these low cytotoxic dyes have potential application in living cell imaging. Furthermore, the effects of different functional groups on the molecule arrangement, ESIPT, AIE, probe, and chiral recognition properties are also examined, which provide a simple and bright paradigm for the design of multiple-stimuli-responsive smart materials.
- Wang, Man,Cheng, Caiqi,Song, Jintong,Wang, Jun,Zhou, Xiangge,Xiang, Haifeng,Liu, Jin
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p. 698 - 707
(2018/06/06)
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- Hypochlorite responsive even hydrazide connecting key and application thereof
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The invention discloses a hypochlorite responsive even hydrazide connecting key and application thereof. A structural formula of the connecting key is (with the reference to the specification); the connecting key is prepared from an R1 parent containing reactive carbonyl and an R2 parent containing reactive carbonyl by a reaction with hydrazine hydrate; the reactive carbonyl can be ester, carboxylic acid, acyl chloride, aldehyde or cyclic ketone. The connecting key can react with specificity of OCl, is oxidized and cut off by OCl to form carboxyl so as to distinguish OCl in ROS, has high specificity, and can be widely used in various fields of hypochlorite response, such as a hypochlorite fluorescent probe, a hypochlorite responsive drug carrier, a hypochlorite responsive nano probe, a prodrug for treating ROS related diseases, a carrier with double effects of diagnosis and treatment and the like.
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Paragraph 0120; 0123-0124
(2019/01/13)
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- A method for synthesizing bromide
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The invention discloses a method for synthesizing bromide of the method, the method is to acetic acid and hydrazine as raw material, the mordenite molecular sieve as catalyst, reaction at certain temperature synthetic bromide. In the reaction system is maintained in excess of hydrazine hydrate, and water generated by the reaction from the reaction system continuously separating out, after the reaction will not participate in the reaction of acetic acid and hydrated [...] out recovery, to take advantage of the heat catalyst is filtered to recover, filtrate cooling crystallization after pure water washing, vacuum drying to obtain bromide finished product. Compared with the prior art, this invention adopts the mordenite molecular sieve as catalyst, the catalytic effect is good, the reaction yield is high, the catalyst is easy to recovery, can be used repeatedly, saves the esterification reaction, the production cost is lowered, the reaction process is no waste and discharge, is an environment-friendly production process.
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Paragraph 0007; 0008; 0009-0011
(2018/07/30)
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- Synthesis of bromide
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The invention discloses a bromide synthesis method, the method is to acetic acid and hydrazine as raw material, the CuO/Cr2 O3 Composite catalyst for reaction at certain temperature synthetic bromide. In the reaction system is maintained in excess of hydrazine hydrate, and water generated by the reaction from the reaction system continuously separating out, effectively promote the reaction of the acid radical jing, shortens the reaction time, improves the reaction yield. Compared with the prior art, this invention adopts the CuO/Cr2 O3 Composite catalyst, good catalytic effect, the reaction yield is high, the catalyst is easy to recovery, can be used repeatedly, the acetic acid is not required to carry out the esterification, shortened the process step, the production cost is reduced, thereby reducing the waste and discharge, is an environment-friendly production process.
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Paragraph 0008; 0009; 0010-0012
(2018/07/30)
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- Synthesis method of acethydrazide
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The invention discloses a synthesis method of acethydrazide. According to the method, acetic acid and hydrazine hydrate are used as raw materials; a ZSM-5 (Zeolite Socony Mobil-5) acid zeolite molecular sieve is adopted as a catalyst; the acethydrazide is synthesized by a reaction at a certain temperature. The hydrazine hydrate is maintained to be excessive in a reaction system; water generated bythe reaction is continuously separated out from the reaction system; the performing of a hydrazidation reaction is effectively promoted; the reaction time is shortened; the reaction yield is improved. Compared with the prior art, the synthesis method adopts the ZSM-5 (Zeolite Socony Mobil-5) acid zeolite molecular sieve as the catalyst, and is good in catalytic effect and high in reaction yield;the catalyst is easily recovered, and can be repeatedly used; the acetic acid does not need to be esterified; process steps are reduced; the production cost is decreased, the discharge of waste is reduced, and the synthesis method is a green and environment-friendly production process.
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Paragraph 0010; 0011; 0012
(2018/07/30)
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- Rescuing the CFTR protein function: Introducing 1,3,4-oxadiazoles as translational readthrough inducing drugs
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Nonsense mutations in the CFTR gene prematurely terminate translation of the CFTR mRNA leading to the production of a truncated protein that lacks normal function causing a more severe form of the cystic fibrosis (CF) disease. About 10% of patients affected by CF show a nonsense mutation. A potential treatment of this alteration is to promote translational readthrough of premature termination codons (PTCs) by Translational Readthrough Inducing Drugs (TRIDs) such as PTC124. In this context we aimed to compare the activity of PTC124 with analogues differing in the heteroatoms position in the central heterocyclic core. By a validated protocol consisting of computational screening, synthesis and biological tests we identified a new small molecule (NV2445) with 1,3,4-oxadiazole core showing a high readthrough activity. Moreover, we evaluated the CFTR functionality after NV2445 treatment in CF model systems and in cells expressing a nonsense-CFTR-mRNA. Finally, we studied the supramolecular interactions between TRIDs and CFTR-mRNA to assess the biological target/mechanism and compared the predicted ADME properties of NV2445 and PTC124.
- Pibiri, Ivana,Lentini, Laura,Melfi, Raffaella,Tutone, Marco,Baldassano, Sara,Ricco Galluzzo, Paola,Di Leonardo, Aldo,Pace, Andrea
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p. 126 - 142
(2018/10/05)
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- Synthesis method of acethydrazide
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The invention discloses a synthesis method of acethydrazide. According to the method, methyl ethyl ketazine and acetamide are used as raw materials to take a reaction at a certain temperature to synthetize the acethydrazide. In the reaction process, excessive methyl ethyl ketazine is added so that the acetamide in a reaction system totally reacts; after the reaction is completed, the acethydrazide is obtained through rectification; the methyl ethyl ketazine is recovered. The method has the advantages that the operation is simple; the reaction yield is high; the energy consumption is low; the post treatment is simple; the product impurities are few; the purity is high; in the reaction process, no waste is discharged; the byproduct recovered ammonia and butanone can be reused for synthesizing the methyl ethyl ketazine; the production cost of the acethydrazide is reduced.
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Paragraph 0008; 0009; 0010
(2017/08/29)
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- A high-efficiency green pymetrozine preparation method
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The invention discloses a high-efficiency and green method for preparing pymetrozine. According to the method, a byproduct methyl acetate produced in a pymetrozine condensation step serves as a raw material and replaces ethyl acetate in a traditional process for synthesizing acethydrazide, and the produced byproduct methanol can serve as a solvent in a subsequent step, so that the byproduct is recycled, and the raw material utilization rate is improved. Hydrogen chloride or concentrated hydrochloric acid in a traditional process is replaced by adopting a saturated hydrogen chloride methanol solution in the condensation step, and moisture in the system is avoided, so that amino triazone is subjected to a hydrolysis reaction, and byproducts are basically eliminated. According to the method, the yield of the product and the utilization rate of the hydrogen chloride are improved, the reaction time is shortened, emission of wastewater and waste gas is reduced, the comprehensive production cost is reduced, and better conditions are created for industrial large-scale production of the product.
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Paragraph 0006; 0030; 0031; 0036; 0037; 0038; 0039
(2017/08/25)
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- Enantioselective Synthesis of 6,6-Disubstituted Pentafulvenes Containing a Chiral Pendant Hydroxy Group
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Simple enantioselective synthesis of 6,6-disubstituted pentafulvenes bearing chiral pendant hydroxy groups are attained by cascade reactivity using commercially available proline-based organocatalysts. Condensation of cyclopentadiene with the acetyl function of a 1,2-formylacetophenone, followed by cyclization of a resulting fulvene-stabilized carbanion with the formyl group, generates bicyclic chiral alcohols with initial er values up to 94:6. Exceptional enantio-enrichment of the resultant alcohols results upon crystallization—even near racemic samples spontaneously de-racemize. This enables new families of substituted cyclopentadienes that are both enantiomerically and diastereomerically pure to be rapidly attained.
- Nouch, Ryan,Cini, Melchior,Magre, Marc,Abid, Mohammed,Diéguez, Montserrat,Pàmies, Oscar,Woodward, Simon,Lewis, William
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supporting information
p. 17195 - 17198
(2017/11/27)
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- Production method of metamitron
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The invention discloses a production method of metamitron. The production method is characterized by comprising the following steps that benzoyl cyanide is hydrolyzed under the condition of H2SO4, and is then alcoholized into ester; hydrazine hydrate and methyl acetate take reaction to generate acetyl hydrazine hydrate; methyl benzoylformate and the acetyl hydrazine hydrate take reaction to generate hydrazine hydrate ester under the condition of H2SO4; hydrazine hydrate ester suspension and hydrazine hydrate take reaction; acyl is subjected to hydrazine treatment again to generate benzoyl hydrazine, and byproducts of methyl alcohol and water are generated; the benzoyl hydrazine is subjected to distillation, backflow, dehydration, cyclization and crystallization under the condition with a butanol solvent and a catalyst to generate the metamitron. The production method has the advantages that the cost of phase transfer catalysts is low; the cost of sodium benzoate is lower than that of sodium acetate, so that the production cost is reduced.
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Paragraph 0037; 0038
(2017/02/17)
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- COMPOUNDS AS HEPATITIS C INHIBITORS AND USES THEREOF IN MEDICINE
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Provided herein are compounds as hepatitis C inhibitors and uses thereof in medicine. Specifically, provided herein is a compound of Formula (I) or a stereoisomer, a tautomer, an enantiomer, an N-oxide, a hydrate, a solvate, a metabolite, a pharmaceutically acceptable salt or a prodrug thereof, which can be used for treating HCV infection or hepatitis C diseases. Also provided herein are a pharmaceutically acceptable composition containing such compound and a method of treating HCV infection or hepatitis C diseases comprising administering the compound or pharmaceutical composition thereof disclosed herein.
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Paragraph 00191
(2016/09/22)
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- Organocatalytic Synthesis of Fused Bicyclic 2,3-Dihydro-1,3,4-oxadiazoles through an Intramolecular Cascade Cyclization
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Hydrazone-carboxylic acids undergo intramolecular cyclization in the presence of pivaloyl chloride, iPr2NEt, and catalytic DABCO to form a range of substituted fused tricyclic 2,3-dihydro-1,3,4-oxadiazoles in high yields.
- Fugard, Alison J.,Thompson, Bethany K.,Slawin, Alexandra M. Z.,Taylor, James E.,Smith, Andrew D.
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supporting information
p. 5824 - 5827
(2015/12/11)
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- Synthesis of 3-hydroxyindanones via potassium salt of amino acid catalyzed regioselective intramolecular aldolization of ortho-diacylbenzenes
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First organocatalytic intramolecular aldolization of ortho-diacylbenzenes to construct highly functionalized 3-hydroxyindanones is described. In this transformation a high trans-selectivity is achieved by the use of metal salt of amino acid. This method allows an easy access to the strained spirocyclic 3-hydroxyindanones related to a number of natural product frameworks. Synthesis of a new class of indole skeleton substituted by 3-hydroxyindanones added an extra essence to this new protocol.
- Chanda, Tanmoy,Chowdhury, Sushobhan,Anand, Namrata,Koley, Suvajit,Gupta, Ashutosh,Singh, Maya Shankar
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supporting information
p. 981 - 985
(2015/03/04)
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- Exploration of fluoral hydrazones derived from carbohydrazides for the synthesis of trifluoromethylated heterocycles
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The reaction of fluoral hydrate with carbohydrazides in methanol in the presence of molecular sieves (4 A) gave the desired N-acylated fluoral hydrazones (3a-f) in fair yields. Treatment of the latter with mercaptoacetic acid in benzene led to the corresponding 2-trifluoromethyl-1,3-thiazolidinone derivatives (4a-f), whereas the reaction with acetic anhydride gave 3-acetyl-2,3-dihydro-2-trifluoromethyl-1,3,4-oxadiazoles (5a-f). The structures of each type of product have been established by X-ray crystallography.
- Mloston, Grzegorz,Urbaniak, Katarzyna,Jacaszek, Natalia,Linden, Anthony,Heimgartner, Heinz
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p. 387 - 401
(2014/01/17)
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- Synthesis of some 1,3,4-thiadiazole derivatives as inhibitors of Entamoeba histolytica
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In the quest for potent anti-amoebic agents, some 1,3,4-thiadiazole derivatives were synthesized and characterized by spectral data. The purity of the compounds was confirmed by elemental analysis. All the compounds were screened in vitro against HM1:IMSS strain of Entamoeba histolytica by microdilution method. The results revealed that compounds 1 (IC50 = 0.670 μM), 3 (IC50 = 1.60 μM) and 8 (IC50 = 0.522 μM) had much better anti-amoebic activity than the reference drug metronidazole (IC50 = 1.80 μM). Further, cytotoxicity of the compounds having IC50 value less than metronidazole was assessed by MTT assay on human breast cancer MCF-7 cell line and all the compounds were found low cytotoxic in the concentration range of 2.5-250 μM. Preliminary results indicate that these three compounds (1, 3 and 8) may be subjected to further investigations and it may be hoped that the present study will stimulate efforts towards the development of novel effective anti-amoebic agents.
- Siddiqui, Shadab Miyan,Salahuddin, Attar,Azam, Amir
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p. 1305 - 1312
(2013/04/10)
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- Synthesis, crystal structure and fungicidal activity of 3-(((4-Cyclopropyl-5-Methyl- 4H-1,2,4-Triazol-3-yl)Thio)Methyl)Benzonitrile H2O (1:1) solvent
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The title compound (C14H14N4S· H2O) were synthesized and recrystallized from ethanol. The compound was characterized by 1H NMR, elemental analyses and X-ray diffraction. The compound crystallized in the monoclinic space group P2(1)/c with a = 11.289(2), b = 15.675(3), c = 8.4835(17) A, α = 90, β = 104.65(3), γ =90°, V = 1452.4(5) A3, Z = 4 and R = 0.0333 for 2545 observed reflections with I > 2σ(I). X-ray analysis reveals that not only intermolecular O-H···N interactions. The biological activities results showed that the title compound exhibited significant fungicidal activity towards six test fungi.
- Jin, Jian-Zhong,Sun, Na-Bo
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p. 955 - 959
(2013/07/26)
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- WNT PATHWAY INHIBITORS
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Wnt pathway inhibitors A class of compounds having general formula (I) has been identified. These compounds function as inhibitors of the Wnt pathway. Compounds of formula (I) are suitable for the treatment and/or prevention of any condition or disease in which it is desirable to inhibit signaling in the Wnt pathway, in particular inhibiting the proliferation of tumor cells, especially those associated with breast cancer, non-small cell lung cancer, pancreatic and colorectal cancers (e.g. colon carcinoma cells). The compounds also find use in methods of preventing metastasis and methods of promoting and/or directing cellular differentiation of progenitor cells.
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Page/Page column 39-40
(2013/07/05)
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- A facile synthesis of pyrimidone derivatives and single-crystal characterization of pymetrozine
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A facile and efficient synthetic methodology for the preparation of aza-pyrimidone and beno-pyrimidone derivatives is described, in which the triazinone ring and dihydroquinazolin-2(1H)-one was convenient constructed. The structures of all the newly synthesized compounds were characterized by mass, 1H NMR, and infrared spectroscopy. In additional, the crystal of pymetrozine was obtained to find useful information such as configuration and molecular action mechanisms.
- Wang, Baozhu,Ke, Shaoyong,Kishore, Babu,Xu, Xiaoyong,Zou, Zhuyan,Li, Zhong
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scheme or table
p. 2327 - 2336
(2012/06/18)
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- Reductive cleavage of amides to alcohols and amines catalyzed by well-defined bimetallic molybdenum complexes
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Triple bonds do it! The molybdenum-catalyzed Ci-N bond cleavage of organic amides with hydrosilanes to produce alcohols and amines has been investigated. This work complements previously established protocols that lead to the cleavage of the Ci-O bond. Modified triply bonded dimolybdenum(III) alkoxides have been found to be crucial for tuning the selectivity to Ci-N bond cleavage (see figure). Copyright
- Krackl, Sebastian,Someya, Chika I.,Enthaler, Stephan
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supporting information
p. 15267 - 15271
(2013/01/15)
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- Synthesis and antifungal activity of 1,2,4-triazole derivatives containing cyclopropane moiety
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A new series of 1,2,4-triazoles containing cyclopropane moiety were synthesized and characterized by 1H NMR and elemental analyses. The biological activities results showed that most of them exhibited significant fungicidal activity towards six test fungi. Among them, several showed superiority over the commercial fungicide during the present study.
- Tan, Cheng-Xia,Shi, Yan-Xia,Weng, Jian-Quan,Liu, Xing-Hai,Li, Bao-Ju,Zhao, Wei-Guang
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experimental part
p. 431 - 435
(2012/07/03)
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- Synthesis of 1,6-hexanediyl-bis(semicarbazides) and 1,6-hexanediyl-bis(1,2, 4-triazol-5-ones) and their antiproliferative and antimicrobial activity
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A series of 1,6-bis(3-substituted 1,5-dihydro-5-oxo-4H-1,2,4-triazol- -4-yl)hexanes 3a-g were synthesized by the cyclization reaction of 1,6-bis{[(2- -substituted hydrazinyl)carbonyl]amino}hexanes 2a-g in alkaline medium. The new derivatives 3a-c were screened in vitro for their antiproliferative and anticancer activity in human tumor cell lines derived from breast and lung carcinoma cells. Compounds 3a (at a concentration of 0.18 mM), 3b (at concentrations of 0.12 and 0.02 mM) and 3c (at concentrations of 0.23 and 0.11 mM) were found to be the most effective against the lung cell line. Compound 3a had the greatest antiproliferative effect on the breast carcinoma cell line. Representative compounds were established and evaluated as antimicrobial agents. All the tested derivatives showed minimum inhibitory concentrations (MIC) in the range 1.87-7.5 μg mL-1. Compound 3b was the most effective against Candida albicans (MIC 1.87 μg mL-1). Copyright 2012 (CC) SCS.
- Pitucha, Monika,Rzymowska, Jolanta,Olender, Alina,Grzybowska-Szatkowska, Ludmia
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scheme or table
p. 1 - 8
(2012/05/05)
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- Application of nickel complexes modified by tridentate O,N,O'-ligands as precatalysts in nickel-catalyzed C(sp2)-C(sp3) bond formations
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1-Acetyl- [1a; 3,5-CF3, 1-C(=O)CH3] and 1-benzoyl-5-hydroxypyrazolines [1b; 3,5-CF3, 1-C(=O)C 6H5] have been synthesized and treated with Ni(OAc) 2·4H2O in the presence of an excess of base [NH3 or 4-(dimethylamino)pyridine (DMAP)] to form the nickel complexes 4a-c. These complexes have been characterized by various techniques, which indicate a tridentate coordination mode of the ligands. X-ray crystallography determined an O,N,O'-coordination of the ligands, in which the ligand is planar, the oxygen donors are trans to each other, and the nitrogen donor is in a cis position. The other coordination sites on the nickel centre are occupied by the added base molecules (NH3 or DMAP). The number of NH3 or DMAP ligands depends on the nature of the base; in the case of ammonia, one molecule is coordinated to the nickel centre to form a diamagnetic square-planar complex, whereas with DMAP, an octahedral paramagnetic complex with three additional DMAP ligands was observed. Initial catalytic experiments have been performed by applying the complexes in the nickel-catalyzed C(sp2)-C(sp3) cross-coupling of aryl halides with benzylzinc bromides or dialkylzinc reagents; excellent yields and selectivities have been achieved.
- Someya, Chika I.,Inoue, Shigeyoshi,Krackl, Sebastian,Irran, Elisabeth,Enthaler, Stephan
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scheme or table
p. 1269 - 1277
(2012/05/19)
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- Synthesis and antihyperlipidemic activity of some novel 4-(substitutedamino)-5-substituted-3-mercapto-(4H)-1,2,4-triazoles
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Hyperlipidemia is considered one of the key factors for cardiovascular diseases. Based on earlier work on a series of 5-alkyl-4-aryl-3-mercapto-(4H)-1, 2,4-triazoles, for further lead modification, a series of 4-(substituted)amino- 5-substituted-3-mercapto-(4H)-1,2,4-triazoles was designed. Target compounds were synthesized by the well known Hoggarth synthesis of substituted 1,2,4-triazoles. Synthesized compounds were screened for lipid lowering activity using the "Poloxamer 407 induced hyperlipidemia in rats" model at a dose of 100 mg/kg p. o. Compounds were found to alter serum lipid levels significantly. Most of the compounds significantly reduced serum cholesterol and triglyceride levels. Some of the compounds were found to reduce triglycerides and elevate high density lipoprotein (HDL) levels more than the standard drug atorvastatin (CAS 134523-03-8). Compounds with chloro substitution on aryl rings were found more active in reducing serum lipid levels than other substitutions. ECV ? Editio Cantor Verlag.
- Chhabria, Mahesh T.,Suhagia, Bhanubhai N.,Brahmkshatriya, Pathik S.,Raval, Priyesha M.
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scheme or table
p. 452 - 457
(2012/06/16)
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- New binding modes of 1-acetyl- and 1-benzoyl-5-hydroxypyrazolines - Synthesis and characterization of O,O′-pyrazoline- and N,O-pyrazoline-zinc complexes
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The 1-acetyl- and 1-benzoyl-5-hydroxypyrazolines 1a [3,5-CF3, 1-C(=O)CH3], 1b [3,5-CH3, 1-C(=O)CH3] and 1c [3,5-CF3, 1-C(=O)C6H5] have been synthesized in good yields and characterized by X-ray crystallography. The 1-acetyl- and 1-benzoyl-5-hydroxypyrazoline ligands were treated with dimethylzinc in a 1:1 molar ratio to form complexes 8 with a RO-Zn-Me motif. These complexes are accessible by simple Bronsted acid-base reactions generating methane as a side product. Characterization of complexes 8a and 8c by X-ray crystallography revealed a dimeric structure in the solid state. The two subunits generate a Zn2O2 square. The acetyl and benzoyl functionality of the ligands coordinate to the metal to span a six-membered ring. Moreover, the coordination mode of the ligand can be easily influenced by the addition of base. Here, N,N,N′,N′-tetramethylethylenediamine (tmeda) was applied to remove the acidic proton in the 4-position of the ligand and to cleave the hemiaminal functional group. The tmeda-H+ transfers the proton to the methyl group connected to the zinc and facilitates the removal of methane; the free tmeda coordinates to the zinc in a bidentate fashion. The positive charge at the zinc and the negative charge in the ligand recombine to form complex 9. Surprisingly, the characterization of complex 9c by X-ray crystallography showed the formation of the first zinc-based seven-membered system with covalent bonding (N1,O6-coordination) in the solid state, whereas for other metals O6,N2,O7-coordination has been reported. The versatility of 5-hydroxypyrazoline ligands has been demonstrated. Various zinc complexes have been synthesized and characterized resulting in new coordination modes of pyrazoline ligands depending on the reaction conditions; zinc dimers havebeen observed with a O,O′-coordination mode, whereas addition of tmeda to the reaction mixture led to the formation of a zinc-containing seven-membered ring system with an O,N-mode. Copyright
- Someya, Chika I.,Inoue, Shigeyoshi,Irran, Elisabeth,Krackl, Sebastian,Enthaler, Stephan
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experimental part
p. 2691 - 2697
(2011/08/02)
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- Synthesis, experimental and theoretical study on the structure of some semicarbazides with potential antibacterial activity
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A series of 1,4-disubstituted semicarbazide and 4,4'-bis[1-substituted semicarbazide]diphenyl-methane derivatives were synthesized to explore their antibacterial activity. New compounds were characterized by elemental analysis and spectroscopic data. In order to find the tautomeric equilibrium for the molecules energy calculations for each possible tautomeric form of model compound 2, and for the most antibacterially active compound 7 in the investigated series, were calculated for the gas phase at the RHF/SCF/6-31G** level of theory.
- Pitucha, Monika,Karczmarzyk, Zbigniew,Kosikowska, Urszula,Malm, Anna
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scheme or table
p. 505 - 511
(2011/06/28)
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- Synthesis and insecticidal activities of 1,3,5-trisubstituted-1,3,5- hexahydrotriazine-2-N-nitroimines
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A new series of 1,3,5-trisubstituted-1,3,5-hexahydrotriazine-2-N- nitroimines (3a-3j) were designed and synthesized as novel neonicotinoid analogues, and their structures were characterized by 1H NMR, IR, elemental analysis and MS. The preliminary bioassay tests showed that most of the target compounds had good insecticidal activities against Nilaparvata lugens as well as Aphis medicaginis at 500 mg/L, while compound 3i had 100% mortality against Nilaparvata lugens at 20 mg/L.
- Xue, Sijia,Ma, Xubo,Bu, Hongfei,Liu, Li,Xu, Xiao
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scheme or table
p. 2153 - 2156
(2012/03/26)
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- Combinatorial synthesis of 3,5-Dimethylene substituted 1,2,4-Triazoles
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Combinatorial cyclizations of imidates and hydrazides with methylene linked R groups, generated from the corresponding nitriles and carboxylic acids, respectively, provided a large library of 3,5-dimethylene substituted 1,2,4- trizoles. 2011 Bentham Science Publishers Ltd.
- Woodard, Scott S.,Jerome, Kevin D.
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experimental part
p. 132 - 137
(2012/04/18)
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- Development and assessment of green synthesis of hydrazides
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An expeditious, solvent free one pot method for the preparation of hydrazides from corresponding acids directly under microwave irradiation is developed. The method has been assessed using green chemistry measures and found superior to conventional method with higher E(environmental) factor, atom economy, atom efficiency, carbon efficiency, reaction mass efficiency.
- Saha, Ajoy,Kumar, Rajesh,Kumar, Rajendra,Devakumar
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experimental part
p. 526 - 531
(2010/10/03)
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- Green synthesis of 5-substituted-1,3,4-thiadiazole-2-thiols as new potent nitrification inhibitors [1]
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(Chemical Equation Presented) A fast, efficient synthesis of 5-substituted-1,3,4-thiadiazole-2-thiols was successfully developed, assessed using green chemistry matrices, and compounds were screened for their in vitro nitrification inhibitory activity. The greener method was superior with higher energy efficiency, E(nvironmental) factor, atom economy, atom efficiency, carbon efficiency, and reaction mass efficiency.
- Saha, Ajoy,Kumar, Rajesh,Kumar, Rajendra,Devakumar
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experimental part
p. 838 - 845
(2010/10/04)
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- NOVEL PYRIMIDINECARBOXAMIDE DERIVATIVES
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This disclosure relates to novel HIV integrase inhibitors their derivatives, pharmaceutically acceptable salts, solvates, and hydrates thereof. This disclosure also provides compositions comprising a compound of this disclosure and the use of such compositions in methods of treating HIV infections.
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Page/Page column 12
(2009/07/02)
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