- Synthesis and X-Ray analysis of new 1,5-benzo-diazepinium picrates
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1,2-Diaminobenzenes react with pentane-2,4-dione in ethanol in the presence of picric acid to give 1,5-benzodiazepinium picrates. In the single crystal, the benzodiazepinium molecules form layers with overlapped 7-membered rings in head-to-tail arrangemen
- Schmidt, Andreas,Shilabin, Abbas Gholipour,Nieger, Martin
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Read Online
- Highly sensitive near-infrared fluorescent probes for nitric oxide and their application to isolated organs
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Novel near-infrared (NIR) fluorescent probes for nitric oxide (NO) have been designed, synthesized, and evaluated. Their NIR fluorescence was increased in an NO concentration-dependent manner under physiological conditions, and their reaction efficiency w
- Sasaki, Eita,Kojima, Hirotatsu,Nishimatsu, Hiroaki,Urano, Yasuteru,Kikuchi, Kazuya,Hirata, Yasunobu,Nagano, Tetsuo
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- A combined mechanochemical and calcination route to mixed cobalt oxides for the selective catalytic reduction of nitrophenols
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Para-, or 4-nitrophenol, and related nitroaromatics are broadly used compounds in industrial processes and as a result are among the most common anthropogenic pollutants in aqueous industrial efiuent; this requires development of practical remediation str
- Shultz, Lorianne R.,McCullough, Bryan,Newsome, Wesley J.,Ali, Haider,Shaw, Thomas E.,Davis, Kristopher O.,Uribe-Romo, Fernando J.,Baudelet, Matthieu,Jurca, Titel
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Read Online
- Liquid-crystalline perylene diester polymers with tunable charge-carrier mobility
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New classes of liquid-crystalline semiconductor polymers based on perylene diester benzimidazole and perylene diester imide mesogens are reported. Two highly soluble side-chain polymers, poly(perylene diester benzimidazole acrylate) (PPDB) and poly(peryle
- Muth, Mathis-Andreas,Carrasco-Orozco, Miguel,Thelakkat, Mukundan
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Read Online
- Galactose Grafted Two-Dimensional Nanosheets as a Scaffold for the In Situ Synthesis of Silver Nanoparticles: A Potential Catalyst for the Reduction of Nitroaromatics
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Two major hurdles in NP-based catalysis are the aggregation of the NPs and their recycling. Immobilization of NPs onto a 2D support is the most promising strategy to overcome these difficulties. Herein, amphiphilicity-driven self-assembly of galactose-hexaphenylbenzene-based amphiphiles into galactose-decorated 2D nanosheet is reported. The extremely dense decoration of reducing sugar on the surface of the sheets is used for the in situ synthesis and immobilization of ultrafine catalytically active AgNPs by using Tollens’ reaction. The potential of the system as a catalyst for the reduction of various nitroaromatics is demonstrated. Enhanced catalytic activity is observed for the immobilized AgNPs when compared to the corresponding discrete AgNPs. Recovery of the catalytic system from the reaction mixture by ultrafiltration and its subsequent recycling for several cycles without dropping its activity is shown. This is the first report demonstrating the in situ synthesis and immobilization of ultrafine AgNPs onto a 2D nanosheet that exhibits excellent catalytic performance for the reduction of nitroaromatics.
- Harikrishnan, Kaloor S.,Krishnan, Nithiyanandan,Kumar, Nilima Manoj,Krishna, Anusree,Raj, Gowtham,Perumal, Devanathan,Kalathil, Jemshiya,Krishna, Jithu,Varghese, Reji
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p. 14100 - 14107
(2021/09/06)
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- Synthesis of CoFe2O4@Pd/Activated carbon nanocomposite as a recoverable catalyst for the reduction of nitroarenes in water
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Efficient reduction of nitro compounds into amines is an important industrial transformation. So, it is a great deal to design new catalysts for efficient reduction of the nitro compounds especially in water. In this work, a new magnetic Pd/activated carbon nanocomposite (CoFe2O4@Pd/AC) was synthesized via metal-impregnation-pyrolysis method. The CoFe2O4@Pd/AC was fully characterized by FT-IR, PXRD, FESEM, TEM, VSM, EDX-mapping and BET techniques. The results showed that CoFe2O4@Pd/AC is a highly reactive and easily recoverable magnetic catalyst for the reduction of the nitro compounds by using NaBH4 in water. For instance, aniline was obtained in high yield (99%) after 75 ?min at 25 ?C by using just 6 ?mg of the catalyst. In addition, CoFe2O4@Pd/AC was recovered by a simple magnetic decantation and it exhibits stable activity and remains intact during the catalytic process with no significant loss in activity (8 cycles).
- Hamadi, Hosein,Kazeminezhad, Iraj,Mohammadian, Sara
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- Design, synthesis and characterization of potent microtubule inhibitors with dual anti-proliferative and anti-angiogenic activities
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Microtubule has been an important target for anticancer drug development. Here we report the discovery and characterization of a series of fused 4-aryl-4H-chromene-based derivatives as highly potent microtubule inhibitors. Among a total of 37 derivatives synthesized, 23 exhibited strong in vitro anti-proliferative activities against A375 human melanoma cells. The relationship between the biological activities of these microtubule inhibitors and their chemical structure variations was analyzed. Studies of compounds 27a, 19a and 9a in parallel with colchicine as the positive control compound in a panel of biological assays revealed that these compounds blocked cell cycle progression, increased apoptosis, and inhibited HUVEC capillary tube formation at low nanomolar concentrations. The most potent compound 27a was also tested in eight additional cancer cell lines besides A375 cells and two non-cancer cells and showed potent and selective activity on these cancer cells. To understand the molecular and structure mechanism of action of these compounds, tubulin polymerization and molecular docking studies were carried out for 27a as the representative. The results were consistent with the mechanism by which 27a interacts with the colchicine binding site on tubulin and disrupts tubulin polymerization. With potent dual actions of microtubule destabilization and vascular disruption described above, this small molecule can serve as a valuable research probe of the function and role of microtubules in human diseases and promising lead for developing new therapeutic agents.
- Zhang, Huijun,Fang, Xiong,Meng, Qian,Mao, Yujia,Xu, Yan,Fan, Tingting,An, Jing,Huang, Ziwei
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supporting information
p. 380 - 396
(2018/08/17)
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- Potent, Selective, and Cell Active Protein Arginine Methyltransferase 5 (PRMT5) Inhibitor Developed by Structure-Based Virtual Screening and Hit Optimization
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PRMT5 plays important roles in diverse cellular processes and is upregulated in several human malignancies. Besides, PRMT5 has been validated as an anticancer target in mantle cell lymphoma. In this study, we found a potent and selective PRMT5 inhibitor by performing structure-based virtual screening and hit optimization. The identified compound 17 (IC50 = 0.33 μM) exhibited a broad selectivity against a panel of other methyltransferases. The direct binding of 17 to PRMT5 was validated by surface plasmon resonance experiments, with a Kd of 0.987 μM. Kinetic experiments indicated that 17 was a SAM competitive inhibitor other than the substrate. In addition, 17 showed selective antiproliferative effects against MV4-11 cells, and further studies indicated that the mechanism of cellular antitumor activity was due to the inhibition of PRMT5 mediated SmD3 methylation. 17 may represent a promising lead compound to understand more about PRMT5 and potentially assist the development of treatments for leukemia indications.
- Mao, Ruifeng,Shao, Jingwei,Zhu, Kongkai,Zhang, Yuanyuan,Ding, Hong,Zhang, Chenhua,Shi, Zhe,Jiang, Hualiang,Sun, Dequn,Duan, Wenhu,Luo, Cheng
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p. 6289 - 6304
(2017/08/02)
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- Effect of Extended Benzannelation Orientation on Bergman and Related Cyclizations of Isomeric Quinoxalenediynes
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A combined computational and experimental study was conducted to examine the effect of extended benzannelation orientation on C1-C5 and C1-C6 cyclization of acyclic quinoxalenediynes. Calculations (mPW1PW91/cc-p
- Valenzuela, Stephanie A.,Cortés, Alondra J.,Tippins, Zakery J. E.,Daly, Morgan H.,Keel, Terell E.,Gherman, Benjamin F.,Spence, John D.
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p. 13297 - 13312
(2017/12/26)
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- Aralkylpiperidine (or piperazinecarboxylic) and its derivatives used for treating hypercalcemia schinzopherenia
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PROBLEM TO BE SOLVED: To provide an agent for treating schizophrenia and related neuropsychiatric diseases.SOLUTION: This invention provides an aralkylpiperidine (or piperazine) derivative represented by formula (1), where A ring is a 5-7 membered heterocycle including N, with the heterocycle including a hetero atom arbitrarily selected from O, S, N; X is O, an amino group or a substituted amino group; Z is CH, N or C; Y is O, N or S; n is an integer of 1-5; and R1-R6 are H, a C1-C4 alkyl group or the like.
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Page/Page column 31
(2018/12/01)
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- A highly efficient oxidative condensation reaction for selective protein conjugation
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We hereby report a mild and efficient coupling reaction between alkyl aldehydes and aryl diamines. In the presence of a Cu2+ or a Zn 2+ ion, oxygen (O2) in air is able to promote the oxidative condensation of the two readily preparable functional groups, forming stable benzimidazole linkages in neutral aqueous solution at room temperature (RT). We demonstrated that the reaction could be utilized to label a T4 lysozyme protein containing a chemically installed aryl diamine group with a fluorescent aldehyde dye molecule at 37 °C. the Partner Organisations 2014.
- Ji, Ao,Ren, Wei,Ai, Hui-Wang
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supporting information
p. 7469 - 7472
(2014/07/07)
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- In situ formed metal nanoparticle systems for catalytic reduction of nitroaromatic compounds
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Developing robust and facile catalytic systems for converting nitroaromatic compounds to NH2-containing compounds are of importance to decrease or even eliminate their toxicity or risk in the environment. In view of in situ formed metal nanoparticles, the metal ion (Cu2+, Ag+, AuCl4-, Co2+ and Ni2+)/NaBH4 systems were employed to catalyze the reduction reaction of nitroaromatic compounds. By employing the reduction of 4-nitrophenol (4-NP) to 4-aminophenol (4-AP) as a model reaction, the effects of concentration of NaBH4, 4-NP and metal ions on the rate constants of the catalytic reduction reactions were systematically investigated. Apparent activation energies of these metal ion/NaBH4 catalytic systems were further measured and compared. In situ formed metal NPs could be characterized by X-ray diffraction (XRD) and transmission electron microscopy (TEM). Furthermore, these metal ion/NaBH4 systems were successfully employed to catalyze the reduction reaction of a series of other nitroaromatic compounds. These metal ion/NaBH4 catalytic systems investigated in this protocol are simple and do not require the preparation of metal nanoparticles in advance, compared with previous related reports. This journal is
- Wu, Xiao-Qiong,Wu, Xing-Wen,Shen, Jiang-Shan,Zhang, Hong-Wu
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p. 49287 - 49294
(2014/12/11)
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- ARALKYL SUBSTITUTED PIPERIDINE OR PIPERAZINE DERIVATIVES AND THEIR USE FOR TREATING SCHIZOPHRENIA
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The present invention discloses an aralkyl substituted piperidine or piperazine derivative and the use of the derivative in preparation of medicaments for treating schizophrenia and correlative psychoneuroses. It is shown by pharmacological tests that the derivative of the present invention has better antischizophrenic effect and less toxicity. Said derivative is a free base or salt of the compound having the following general formula.
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Page/Page column 26
(2011/06/10)
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- Convenient reduction of nitro compounds to their corresponding amines with promotion of NaBH4/Ni(OAc)2.4H2O system in wet CH3CN
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NaBH4 in the presence of catalytic amounts of Ni(OAc) 2.4H2O reduces varieties of nitro compounds to their corresponding amines. Reduction reactions were carried out in a mixture of CH3CN and H2O (3.0:0.3 ml) at room temperature with high to excellent yields of products.
- Setamdideh, Davood,Khezri, Behrooz,Mollapour, Manouchehr
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experimental part
p. 991 - 996
(2012/03/27)
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- Rapid and efficient reduction of nitroarenes to their corresponding amines with promotion of NaBH4/NiCl2·6H2O system in aqueous CH3CN
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NaBH4 in the presence of catalytic amounts of NiCl2 6H2O reduces varieties of nitroarenes to their corresponding amines. Reduction reactions were carried out in a mixture of CH3CN and H 2O (3.0:0.3 mL) at room temperature with high to excellent yields of products.
- Setamdideh, Davood,Khezri, Behrooz
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scheme or table
p. 5575 - 5580
(2012/07/31)
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- A mild and convenient reduction of nitro compounds with NaBH 4/SbF3 system in wet CH3CN
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NaBH4 in the presence of catalytic amounts of SbF3 reduces a range of nitro compounds to their corresponding amines in high to excellent yields. Reduction reactions were carried out in wet CH3CN within 2-30 minutes at room temperature.
- Zeynizadeh, Behzad,Ghasemi, Hamed
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p. 542 - 544
(2007/10/03)
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- AMINO-BENZAZOLES AS P2Y1 RECEPTOR INHIBITORS
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The present invention provides novel amino-benzazoles and analogues thereof, which are selective inhibitors of the human P2Y1 receptor. The invention also provides for various pharmaceutical compositions of the same and methods for treating dis
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Page/Page column 113-114
(2008/06/13)
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- One step hair coloring compositions using salts
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A hair coloring composition comprising the following two compositions which are mixed just prior to application to the hair: (a) a composition comprising a water-soluble peroxygen oxidizing agent; and (b) a composition comprising one or more oxidative hair coloring agents selected from the group consisting of an aromatic diamine, an amino phenol, a naphthol, a polyhydric phenol, a catechol and mixtures thereof; wherein the composition comprising one or more oxidative hair coloring agents further comprises al least one water soluble carbonate releasing salts; and optionally a water soluble ammonium salt, is described.
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- On benzo[b][1,4]diazepinium-olates, -thiolates and -carboxylates as anti-Hueckel mesomeric betaines
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2,3-Diaminophenol 4, 3,4-diaminophenol 5, 4-methoxy-1,2-diaminobenzene 6, 3,4-diaminobenzenthiol 7, 2,3-diaminobenzoic acid 8, and 3,4-diaminobenzoic acid 9 were reacted with 2,4-pentanedione to yield the corresponding benzo[b][1,4]diazepinium salts, respectively. The hydroxy-benzo[b][1,4]diazepinium salts 17 and 18 do not form mesomeric betaines (MB) on deprotonation. Instead, they are converted into the diimines 24 and 25. By contrast, the 7-mercaptobenzo[b][1,4]diazepinium salt 20 yields the corresponding thiolate on increasing the pH of the solution. This MB, which possesses 4n π-electrons, does not fit into the classification system of heterocyclic mesomeric betaines accepted today. Deprotonation of the betaine results in the formation of an instable anionic thiolate 31 which oxidizes immediately to the disulfide 32. The carboxy derivatives 21 and 22 readily form cross-conjugated mesomeric betaines. Whereas the diimine 34 proved to be instable, the sodium salt of the diimine 36 was unambiguously characterized. An X-ray single crystal analysis of 22 as its picrate is presented in order to gain additional insights into these 4n π-electron systems.
- Schmidt, Andreas,Gholipour Shilabin, Abbas,Nieger, Martin
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p. 4342 - 4350
(2007/10/03)
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- Hair conditioning compositions and their use in hair colouring compositions
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The present invention relates to a hair care composition comprising a aminofunctional polysiloxane having a specified average effective particle size which provides improved durable conditioning particularly when utilised in conjunction with a hair colouring composition.
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- Transition metal complexes as dye forming catalysts in hair coloring compositions
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A hair coloring composition comprising a first composition which comprises: (a) a dye forming transition metal salt or complex; which is first applied to the hair; and a second composition which comprises the following two compositions which are mixed just prior to application to the hair: (a) a composition comprising a water-soluble peroxygen oxidizing agent; and (b) a composition comprising one or more oxidative hair coloring agents selected from the group consisting of an aromatic diamine, an aminophenol, a polyhydric phenol a catechol and mixtures thereof.
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- Enhanced color deposition for hair with sequestering agents
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Hair coloring compositions which comprise: (A) non-nitrogenous chelating agents from the group consisting of polyphosphate; phosphonates; hydroxycarboxylates; polyacrylates; zeolite; and mixtures thereof; (B) an oxidative dye primary intermediate; and (C) an oxidative dye coupler; (D) and water are described. The present invention also relates to a method for coloring hair which comprises contacting said hair with a hair coloring composition as described above.
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- Hair colouring and conditioning compositions
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A hair colouring and conditioning composition comprising: (a) a hair colouring agent; and (b) a hair conditioning agent; wherein the composition provides an Average Combing Index Value of greater than 1.2 as measured by the Combing Technical Test Method. The products can provide excellent hair colouring together with excellent conditioning, reduced hair damage, brittleness and dryness, and is convenient and easy to use.
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- HAIR COLORING COMPOSITIONS
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A hair coloring composition comprising: (a) from about 0.0003 moles (per 100 g of composition) to less than about 0.09 moles (per 100 g of composition) of an inorganic peroxygen oxidizing agent; and (b) an oxidative hair coloring agent; wherein the pH of each of (a) and (b) is in the range of from about 1 to about 6 and wherein the combined mixture of (a) and (b) has a pH in the range of from about 1 to about 6. The products can provide excellent hair coloring and in-use efficacy benefits including excellent initial color and good wash fastness in combination with reduced hair damage at low pH.
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- HAIR COLORING COMPOSITIONS
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A hair coloring composition comprising: (a) a preformed organic peroxyacid oxidising agent; and (b) an oxidative hair coloring agent; wherein the pH of each of components (a) and (b) is in the range of from about pH 1 to less than about pH 7 and wherein the pH of the composition is in the range of from about pH 1 to less than about pH 7. The products can provide excellent hair coloring and in-use efficacy benefits including excellent initial color and good wash fastness in combination with reduced hair damage at low pH.
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- Novel compounds and compositions for treating diseases asociated with protease activity
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Novel compounds, compositions and methods effective for the prevention and treatment of mast-cell mediated inflammatory disorders are described. The compounds, compositions and methods are effective for the prevention and treatment of inflammatory diseases associated with the respiratory tract, such as asthma and allergic rhinitis, as well as other types of immunomediated inflammatory disorders, such as rheumatoid arthritis, conjunctivitis and inflammatory bowel disease, various dermatological conditions, as well as certain viral conditions. The compounds comprise potent and selective inhibitors of the mast cell protease tryptase. The compositions for treating these conditions include oral, inhalant, topical and parenteral preparations as well as devices comprising such preparations.
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- Design, synthesis, and in vitro biological activity of benzimidazole based Factor Xa inhibitors
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Inhibitors based on the benzimidazole scaffold showed subnanomolar potency against Factor Xa with 500-1000-fold selectivity against thrombin and 50-100-fold selectivity against trypsin. The 2-substituent on the benzimidazole ring had a strong impact on th
- Zhao, Zuchun,Arnaiz, Damian O.,Griedel, Brian,Sakata, Steven,Dallas, Jerry L.,Whitlow, Marc,Trinh, Lan,Post, Joseph,Liang, Amy,Morrissey, Michael M.,Shaw, Kenneth J.
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p. 963 - 966
(2007/10/03)
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- NAPHTHYL-SUBSTITUTED BENZIMIDAZOLE DERIVATIVES AS ANTICOAGULANTS
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Compounds of formula (I): STR1 wherein: n,A,R 1,R 2,R 3, and R 4 have meanings as defined herein, or a pharmaceutically acceptable salt thereof, are useful as anti-coagulants.
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- New low-density lipoprotein receptor upregulators acting via a novel mechanism
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The synthesis and biological activity of a new series of benzamides and related compounds that upregulate the expression of the low-density lipoprotein (LDL) receptor in human hepatocytes (HepG2 cells) by a novel mechanism are described. The lead compound, N-[5-[(3- cyclohexylpropionyl)amino]-2-methylphenyl]-4-hydroxybenzamide (1, RPR102359), increased the expression of the LDL receptors in HepG2 cells by 80% when tested at a concentration of 3 μM. Mevinolin (lovastatin) was found to increase the LDL receptor expression by 70% at the same concentration. In contrast to mevinolin, 1 was found to have no effect on cholesterol biosynthesis in liver homogenates or in HepG2 cells at doses where substantial upregulation of the LDL receptor was observed and thus stimulated LDL receptor expression by a novel mechanism.
- Ashton, Michael J.,Brown, Thomas J.,Fenton, Garry,Halley, Frank,Harper, Mark F.,Lockey, Peter M.,Porter, Barry,Roach, Alan G.,Stuttle, Keith A. J.,Vicker, Nigel,Walsh, Roger J. A.
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p. 3343 - 3356
(2007/10/03)
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- New heterocyclic derivatives of benzimidazole with germicidal activity - XI - Experimental validation of QSAR prediction on antibacterial and antimycotic activity of benzimidazole derivatives
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In continuation of previous studies, the authors describe the synthesis of three new derivatives of 2-(5'-nitro-2'-furyl) benzimidazole, having hydroxy, methoxy or amino group at position 5. The new compounds, synthesized as suggested by a previous chemometric study, were tested in vitro against 5 Gram+ and 4 Gram- strains and the mycete C. albicans. Two derivatives (R = OH, NH2) showed a good degree of antibacterial activity, especially the 5-hydroxy derivative, but they were practically inactive against the mycete; these results are in agreement with the prediction of chemometric study.
- Pedini,De Meo,Ricci,Bastianini
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p. 671 - 674
(2007/10/02)
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- STUDY OF ELECTROPHILIC SUBSTITUTION AND OXIDATION REACTIONS OF 4- AND 5-HYDROXYBENZO-2,1,3-SELENADIAZOLES
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The halogenation, nitrosation, and oxidation of 4- and 5-hydroxybenzo-2,1,3-selenadiazoles have been studied, as has the acetylation of these hydroxy compounds and their halogen and nitroso derivatives.The structure of the resulting compounds has been demonstrated, and it has been found that the nitroso-substituted derivatives exist primarily in the tautomeric oxime form.
- Belen'kaya, I. A.,Sirik, S. A.,Shapiro, Yu. E.,D'yachenko, E. K.
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p. 956 - 961
(2007/10/02)
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- Process for the manufacture of benzimidazolones-(2)
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Process for the manufacture of benzimidazolones-(2) wherein an o-phenylenediamine is reacted with optionally alkylated urea in the ratio of 1 to 1.3 moles per mole o-phenylenediamine in an organic solvent which has a solubility in water of not more than 5 g/l and has a boiling point above 100° C, at a temperature between 100° and 200° C.
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- Enzyme-activated oxidative process for coloring hair
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An enzyme-based oxidative process for coloring hair wherein the hair is exposed to a solution having a pH of about 4 to about 10 and containing hydrogen peroxide, soybean peroxidase enzyme and one or more oxidation dye precursors.
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- Perfluoroalkyl benzodiazepines
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New perfluoroalkyl derivatives of benzodiazepine are prepared by reacting an orthophenylenediamine with a beta-diketone at least one of whose alkyls is a C1 - C15 perfluoroalkyl. The stable products are useful as heat-exchange substances and as surfactants in organic solution.
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