- Synthesis, Crystal Structure, Fluorescent and Antioxidation Properties of Cerium(III) and Europium(III) Complexes with Bis(3-methoxysalicylidene)-3-oxapentane-1,5-diamine
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Two aliphatic ether Schiff base lanthanide complexes (Ln = Eu, Ce) with bis(3-methoxysalicylidene)-3-oxapentane-1,5-diamine (Bod), were synthesized and characterized by physicochemical and spectroscopic methods. [Eu(Bod)(NO3)3] (1) is a discrete mononuclear species and [Ce(Bod)(NO3)3DMF]∞ (2) exhibits an inorganic coordination polymer. In the two complexes, the metal ions both are ten-coordinated and the geometric structure around the LnIII atom can be described as distorted hexadecahedron. Under excitation at room temperature, the red shift in the fluorescence band of the ligand in the complexes compared with that of the free ligand can be attributed to coordination of the rare earth ions to the ligand. Moreover, the antioxidant activities of the two complexes were investigated. The results demonstrated that the complexes have better scavenging activity than both the ligand and the usual antioxidants on the hydroxyl and superoxide radicals.
- Tang, Xia,Shi, Xinkui,Xu, Yuling,Shen, Kesheng,Mao, Shanshan,Wu, Huilu
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- Enhancing insulin sensitivity by dual PPARγ partial agonist, β-catenin inhibitor: Design, synthesis of new αphthalimido-o-toluoyl2-aminothiazole hybrids
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Aims: Partial PPARγ agonists attracted substantially heightened interest as safer thiazolidinediones alternatives. On the other hand, Wnt/β-catenin antagonists have been highlighted as promising strategy for type 2 diabetes management via up-regulating PPARγ gene expression. We aimed at synthesizing novel partial PPARγ agonists with β-catenin inhibitory activity which could enhance insulin sensitivity and avoid the side effects of full PPARγ agonists. Main methods: We synthesized novel series of α-phthlimido-o-toluoyl-2-aminothiazoles hybrids for evaluating their antidiabetic activity and discovering its mechanistic pathway. We assessed effect of the new hybrids on PPARγ activation using a luciferase reporter assay system. Moreover, intracellular triglyceride levels, gene levels of c/EBPα, PPARγ and PPARγ targets including GLUT4, adiponectin, aP2 were measured in 3T3-L1 cells. Uptake of 2-DOG together with PPARγ and β-catenin protein levels were evaluated in 3T3-L1cells. In addition, molecular docking studies with PPARγ LBD, physicochemical properties and structure activity relationship of the novel hybrids were also studied. Key findings: Three of the synthesized hybrids showed partial PPARγ agonistic activity and distinct PPARγ binding pattern. These compounds modulated PPARγ gene expression and PPARγ target genes; and increased glucose uptake in 3T3-L1 and slightly induced adipogenesis compared to rosiglitazone. Moreover, these compounds reduced β-catenin protein level which reflected in increased both PPARγ gene and protein levels that leads to improved insulin sensitivity and increased GLUT4 and adiponectin gene expression. Significance: Our synthesized compounds act as novel partial PPARγ agonists and β-catenin inhibitors that have potent insulin sensitizing activity and mitigate the lipogenic side effects of TZDs.
- Mourad, Ahmed A. E.,Mourad, Mai A. E.
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- Synthesis and Characterization of Novel Phthalimide-pyrano[3,2-c]chromene and Phthalimide-pyrano-2-one Hybrids
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Coumarin skelton holds substantial promise for further exploration because of its immense pharmacological potential. In this pursuit, a series of phthalimide-chromen and phthalimide-pyran-2-one hybrids were synthesized in efficient yields via one-pot multicomponent reaction of aldehyde linked to phthalimide moiety, 4-hydroxy coumarin/4-hydroxy-6-methyl-2H-pyran-2-one, and malanonitrile by Knoevenagel reaction at room temperature in the presence of DABCO as catalyst. The compounds were characterized by 1H NMR and 13C NMR, MS, and FTIR. All the compounds consisting of phthalimide-chromen/pyrano-2-one moieties tethered by spacers of varying lengths were evaluated for their biological activity in Ellman's assay. Most of the compounds feebly inhibited Acetylcholinesterase Enzyme and were inactive toward Butyrylcholinesterase Enzyme.
- Sameem, Bilqees,Saeedi, Mina,Mahdavi, Mohammad,Nadri, Hamid,Vafadarnejad, Fahimeh,Amini, Mohsen
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- A mesogenic triphenylene-perylene-triphenylene triad
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A straightforward synthesis of triphenylene-perylene-triphenylene triad structures has been achieved by using versatile triphenylene intermediates bearing a single oxyalkyl amine side chain. Among these, PBITP10 showed a stable columnar mesophase implying favorably matched core-core separations in the structure. Importantly, the triad can be used as a vehicle for doping columnar triphenylene matrices with functional but incompatible perylene units and a mixture of hexahexyloxytriphenylene matrix doped with 0.1% PBITP10 is homogeneous and liquid crystalline.
- Kong, Xiangfei,He, Zhiqun,Zhang, Yinning,Mu, Linping,Liang, Chunjun,Chen, Bo,Jing, Xiping,Cammidge, Andrew N.
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- Redox-active binary eutectics: Preparation and their electrochemical properties
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Eutectics are emerging as promising candidate for electrochemical energy storage. However, the eutectics usually show high viscosity that usually arises from strong intermolecular interactions greatly limits their application. In this communication, we design and prepare two redox-active molecules that both are able to form binary eutectics with TBMA-TFSI. Combined experimental and computational studies indicate the intermolecular interaction is weakened after eutectic formation, resulting in decreased viscosity and enhanced ionization ratio of TBMA-TFSI without affecting the redox behaviors of the individual molecules. Further, the redox-active binary eutectic is used as solvent-free electrolyte for battery application.
- Chen, Hui,Niu, Zhihui,Zhao, Yu
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- Monofluorinated Nitrogen Containing Heterocycles: Synthesis, Characterization and Fluorine Effect
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A straight forward synthesis and efficient introduction of fluoromethyl group in nitrogen heterocycles is reported. Starting from the respective NH heterocycles fluoromethylation is performed with fluoroiodomethane and proceeds under mild reaction conditions. Structural information of monofluoromethylated nitrogen-containing cyclic compounds containing the biologically active NCH2F moiety are reported. The particularly impressively change of physical and spectroscopic properties by the substitution of a methyl group by a monofluoromethyl group is discussed based on these examples.
- Reichel, Marco,Karaghiosoff, Konstantin
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- Design, synthesis and preliminary bioactivity evaluation of bitopic benzopyranomorpholine analogues as selective dopamine D3 receptor ligands as anti-drug addiction therapeutic agents
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Three series of bitopic benzopyranomorpholine analogues were designed, synthesized, and evaluated as a novel class of selective ligands for the dopamine D3 receptor. Binding affinities of target compounds were determined using the method of radioligand binding assay. Most compounds demonstrated considerable binding affinities and selectivity for D3 receptor. Besides, the compounds were screened for their ability to alleviate withdrawal symptoms of opioid addiction in animal behavioral models. The results showed that compound 20h displayed nanomolar affinity for the D3R, and exhibited anti-drug addiction efficacy in the animal model of of naloxone-induced withdrawal symptoms in morphine-dependent mice.
- Cai, Jin,Chen, Xixi,Huang, Mingqi,Ji, Min,Wang, Yuhong
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- SYNTHESIS OF 2-(2-AMINOETHOXY) ETHANOL
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A method for synthesizing 2-(2-aminoethoxy) ethanol, including the steps of producing 2-(2-phthalimidoethoxy) ethanol by reacting 5-tosyloxy-3-oxapentanol with potassium phthalate and converting the 2-(2-phthalimidoethoxy) ethanol to the 2-(2-aminoethoxy) ethanol by reacting the 2-(2-phthalimidoethoxy) ethanol with hydrazine monohydrate. Reacting the 2-(2-phthalimidoethoxy) ethanol with the hydrazine monohydrate may include forming a final mixture by adding the hydrazine monohydrate to a solution of 2-(2-phthalimidoethoxy) ethanol, refluxing the final mixture in a nitrogen atmosphere, extracting a second organic phase containing the 2-(2-aminoethoxy) ethanol from the final mixture using a second portion of chloroform, and purifying the 2-(2-aminoethoxy) ethanol from the second organic phase.
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Paragraph 0061-0062
(2021/02/12)
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- Dinotefuran hapten, colloidal gold labeled dinotefuran monoclonal antibody and dinotefuran colloidal gold detection device (by machine translation)
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The invention belongs to the technical field of biological detection, and particularly relates to a dinotefuran hapten and dinotefuran colloidal gold detection device and a preparation method thereof. Compared with the prior art, the dinotefuran colloidal gold detection device has the advantages of being convenient to use, economical, rapid, easy to manufacture and low in cost. (by machine translation)
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Paragraph 0029; 0033-0035; 0043
(2020/09/20)
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- BIOISPIRED PROTEASOME ACTIVATORS WITH ANTIAGEING ACTIVITY
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The present invention relates to novel bio-inspired hybrid compounds of formula I which act as proteasome activators and exhibit anti-ageing activity, as well as methods for their synthesis. These hybrid compounds combine the structural features of hydroxytyrosol and the natural antioxidant vitamin E or its bioisosteres in one molecular scaffold. The compounds of formula I, which include structural proteasome activators (activation by stereochemical interaction), can be used in the production of anti-ageing products, such as cosmetic preparations. Additionally, they can be used in conditions and diseases where the proteasome is down-regulated, as well as proteasome-activation control compounds.
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Page/Page column 7; 19
(2019/10/01)
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- APOPTOSIS SIGNAL-REGULATING KINASE INHIBITORS AND USES THEREOF
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Described herein are ASK1 inhibitors and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for the treatment of blood disease, autoimmune disorders, pulmonary disorders, hypertension, inflammatory diseases, fibrotic diseases, diabetes, diabetic nephropathy, renal diseases, respiratory diseases, cardiovascular diseases, acute lung injuries, acute or chronic liver diseases, and neurodegenerative diseases.
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Paragraph 00230; 00228
(2019/04/09)
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- Delta-aminoalkylbenzofuranol ethers, and preparation method and application thereof
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The invention relates to delta-aminoalkylbenzofuranol ethers represented by chemical structural formula I shown in the description, and an application thereof in the preparation of herbicides. In thechemical structural formula I, R is selected from C1-C2 alkyl groups, and n is selected from 2, 3 and 4.
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Paragraph 0020-0024
(2018/04/01)
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- Synthesis of [13C3]-B6 vitamers labelled at three consecutive positions starting from [13C3]-propionic acid
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[13C3]-labelled vitamers (PN, PL and PM) of the B6 group were prepared starting from [13C3]-propionic acid. [13C3]-PN was synthesized in ten linear steps with an overall yield of 17%. Hereby, higher alkyl homologues of involved esters showed a positive impact on the reaction outcome of the intermediates in the chosen synthetic route. Oxidation of [13C3]-PN to [13C3]-PL was undertaken using potassium permanganate and methylamine followed by acid hydrolysis of the imine derivative. [13C3]-PM could be prepared from the oxime derivative of [13C3]-PN by hydrogenation with palladium.
- Bachmann, Thomas,Rychlik, Michael
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- Endoperoxide-8-aminoquinoline hybrids as dual-stage antimalarial agents with enhanced metabolic stability
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Hybrid compounds may play a critical role in the context of the malaria eradication agenda, which will benefit from therapeutic tools active against the symptomatic erythrocytic stage of Plasmodium infection, and also capable of eliminating liver stage parasites. To address the need for efficient multistage antiplasmodial compounds, a small library of 1,2,4,5-tetraoxane-8- aminoquinoline hybrids, with the metabolically labile C-5 position of the 8-aminoquinoline moiety blocked with aryl groups, was synthesized and screened for antiplasmodial activity and metabolic stability. The hybrid compounds inhibited development of intra-erythrocytic forms of the multidrug-resistant Plasmodium falciparum W2 strain, with EC50 values in the nM range, and with low cytotoxicity against mammalian cells. The compounds also inhibited the development of P. berghei liver stage parasites, with the most potent compounds displaying EC50 values in the low μM range. SAR analysis revealed that unbranched linkers between the endoperoxide and 8-aminoquinoline pharmacophores are most beneficial for dual antiplasmodial activity. Importantly, hybrids were significantly more potent than a 1:1 mixture of 8-aminoquinoline-tetraoxane, highlighting the superiority of the hybrid approach over the combination therapy. Furthermore, aryl substituents at C-5 of the 8-aminoquinoline moiety improve the compounds' metabolic stability when compared with their primaquine (i.e. C-5 unsubstituted) counterparts. Overall, this study reveals that blocking the quinoline C-5 position does not result in loss of dual-stage antimalarial activity, and that tetraoxane-8- aminoquinoline hybrids are an attractive approach to achieve elimination of exo- and intraerythrocytic parasites, thus with the potential to be used in malaria eradication campaigns.
- Capela, Rita,Magalh?es, Joana,Miranda, Daniela,Machado, Marta,Sanches-Vaz, Margarida,Albuquerque, Inês S.,Sharma, Moni,Gut, Jiri,Rosenthal, Philip J.,Frade, Raquel,Perry, Maria J.,Moreira, Rui,Prudêncio, Miguel,Lopes, Francisca
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supporting information
p. 69 - 78
(2018/03/06)
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- A high-purity phthalimide potassium salt production method
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The invention discloses a method for producing a high-purity phthalimide potassium salt. With phthalimide and potassium alcoholate as raw materials, phthalimide potassium salt is synthesized in an alcoholic solution. A reaction system does not generate water, so that generation of a by-product o-acylamino potassium benzoate can be avoided, and thus the high-purity phthalimide potassium salt is obtained. The production method disclosed by the invention is simple to operate; the purity of the product can reach over 99%; and the production requirements of high-purity medicines can be met.
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Paragraph 0018-0019; 0021; 0023
(2017/08/26)
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- N-(4-alkyl-5-benzylthiazol-2-yl)aminoalkylamide, and preparation method and application thereof
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The invention relates to N-(4-alkyl-5-benzylthiazol-2-yl)aminoalkylamide with a chemical structural formula I as described in the specification or salts thereof. In the formula I, R is selected from a group consisting of C1-C2 alkyl groups, C3-C4 straight-chain alkyl groups and C3-C4 branched-chain alkyl groups; Y and Y are selected from a group consisting of hydrogen, a methyl group, an ethyl group, a hydroxyl group, a methoxy group, an ethoxy group, fluorine, chlorine, bromine and iodine; Y and Y are selected from a group consisting of hydrogen, a methyl group and an ethyl group; n is in a range of 1 to 9; and the salt is selected from a group consisting of hydrochloride, hydrobromide, sulfate, nitrate, phosphate, mesylate, benzene sulfonate, tosilate, malate, lactate, succinate, maleate and fumarate. The invention also discloses application of N-(4-alkyl-5-benzylthiazol-2-yl)aminoalkylamide or the salts thereof to preparation of anticancer drugs.
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Paragraph 0051; 0052
(2017/07/19)
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- N-[(dihydrobenzofuran-7-yloxyl)alkyl]-2-aryloxy amide derivatives
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The invention discloses N-[( dihydrobenzofuran-7-yloxyl)alkyl]-2-aryloxy amide derivatives which are represented as a structural formula I and a structural formula II, and in the structural formula I or II, R is selected from a group consisting of H, C1-C2 alkyl, C3-C4 linear alkyl and C3-C4 branched alkyl; n is selected from a group consisting of 1,2,3,4,5 and 6; Y is selected from a group consisting of H, C1-C2 alkyl, F, Cl, Br and I; Y is selected from a group consisting of H, C1-C2 alkyl, F, Cl, Br, I, trifluoromethyl and trifluoroethyl; and Y is selected from a group consisting of H, C1-C2 alkyl, F, Cl, Br and I. The invention also provides an application of the N-[(dihydrobenzofuran-7-yloxyl)alkyl]-2-aryloxy amide derivatives to preparing herbicides.
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Paragraph 0027; 0028; 0029; 0030
(2017/12/27)
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- A phthalimide derivative and its preparation method and application
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The invention belongs to the technical field of insect killing and sterilization of chemical pesticides, and in particular relates to phthalimide derivatives as well as a preparation method and application thereof. The phthalimide derivatives can be prepared from raw materials such as phthalimide, potassium hydroxide, dibromoalkane, substituted piperazinyl phenol, acyl chloride (phosphoryl chloride) and the like by virtue of multi-step chemical reactions. The phthalimide derivatives disclosed by the invention can be used for killing insects such as aphids, cabbage worms, plant hoppers, thrips, tetranychus cinnabarinus, root-knot nematodes and the like, also have certain sterilization and bacterium inhibition effects, can be used for effectively controlling plant inset pests, harmful mites, nematodes and harmful bacteria, and can also be applied to prevention and control of diseases, insect pests and pathogenic bacteria in agriculture.
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Paragraph 0039
(2017/08/24)
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- Triphenylene-perylene monoimide diformate binary compound, preparation method and applications thereof
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The present invention provides a triphenylene-perylene monoimide diformate binary compound, which has a structure represented by a general formula I. The present invention further provides a preparation method of the triphenylene-perylene monoimide diformate binary compound, and applications of the triphenylene-perylene monoimide diformate binary compound as an organic solar cell active layer. Compared to the compound in the prior art, the compound of the present invention has advantages of easy adjustment of liquid crystal phase change temperature and temperature range, such that the compound has optical, electronic and electro-optical uses, and especially has uses as the organic solar cell active layer. The general formula (I) is defined in the specification.
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Paragraph 0078; 0079; 0080
(2016/10/08)
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- A kind of amino acid- the amine decorates composition and its preparation method and application
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The invention belongs to the field of medicinal chemistry and in particular relates to amino acid-amine conjugate and a preparation method and application thereof. A general formula of the amino acid-amine conjugate is shown in the specification. According to the amino acid-amine conjugate, amino acid and amine are combined together, the water solubility, biological properties and drug targeting of amine compounds can be improved, and anti-cancer targeting can be realized.
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Paragraph 0027; 0058; 0060
(2017/04/05)
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- USE OF SATURATED AMINE COMPOUNDS IN PREPARING MEDICINES TO RESIST RADIATION DAMAGE AND PROMOTE REGENERATION AND REPAIR OF RADIATION-DAMAGED TISSUES
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Disclosed in the present invention is new use of saturated amine compounds for use in preparing medicines to resist radiation damage and promoting regeneration and repair of radiation-damaged tissues. Experiments show that the saturated amine compounds can increase the counts of white blood cells (WBC), red blood cells (RBC) and platelets (PLT) in the peripheral blood of radiation-damaged animals, promote multiplication of bone marrow hematopoietic stem/progenitor cells and restoration of the hematopoietic system, and bring favorable reparative effects to the intestinal, hepatic and pulmonary tissues of radiation-damaged mice, thus significantly improving the survival rate of radiation-damaged animals.
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- Synthesis, structure, antioxidation, and DNA-binding studies of a binuclear ytterbium(III) complex with bis(N-salicylidene)-3-oxapentane-1,5-diamine
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A new complex of ytterbium(III) nitrate with bis(N-salicylidene)-3-oxapentane-1,5-diamine (H2L), with the composition Yb2(L)2(NO3)2·2H2O, was synthesized and characterized by physic-chemical and spectroscopic methods. The crystal structure of the ytterbium(III) complex has been determined by single-crystal X-ray diffraction. It reveals a centrosymmetric binuclear neutral entity where Yb(III) metal centers are bridged by two phenoxo oxygen atoms. Electronic absorption titration spectra, ethidium bromide displacement experiments, and viscosity measurements indicate that both the ligand and the Yb(III) complex can bind calf thymus DNA, presumably via a groove binding mechanism. Furthermore, the antioxidant activities of the Yb(III) complex were determined by a superoxide and hydroxyl radical scavenging method in vitro, which indicates that it is a scavenger for OH and O2 - radicals.
- Wu, Huilu,Pan, Guolong,Bai, Yuchen,Wang, Hua,Kong, Jin,Shi, Furong,Zhang, Yanhui,Wang, Xiaoli
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p. 3375 - 3388
(2015/06/08)
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- Equimolar carbon absorption by potassium phthalimide and in situ catalytic conversion under mild conditions
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Potassium phthalimide, with weak basicity, is an excellent absorbent for rapid carbon dioxide capture with almost equimolar absorption. This process is assumed to proceed through the potassium carbamate formation pathway, as supported by NMR spectroscopy, an in situ FTIR study, and computational calculations. Both the basicity and nucleophilicity of phthalimide salts have a crucial effect on the capture process. Furthermore, the captured carbon dioxide could more easily be converted in situ into value-added chemicals and fuel-related products through carbon capture and utilization, rather than going through a desorption process. In a fix: Potassium phthalimide is as an excellent absorbent for equimolar CO2 capture with simultaneous activation. The in situ catalytic conversion of captured CO2 can be successfully converted into value-added chemicals and fuel-related products under mild conditions through a carbon capture and utilization pathway, rather than going through desorption process.
- Zhang, Shuai,Li, Yu-Nong,Zhang, Ya-Wei,He, Liang-Nian,Yu, Bing,Song, Qing-Wen,Lang, Xian-Dong
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p. 1484 - 1489
(2014/06/09)
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- USE OF SATURATED AMINES COMPOUNDS IN MANUFACTURE OF MEDICAMENTS FOR MOBILIZING PERIPHERAL BLOOD HEMATOPOIETIC STEM CELL
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The invention provides a new use of a saturated amine compound, i.e., in manufacture of peripheral blood hematopoietic stem cell mobilizing agents. Experiments show that this compound (Code No. TA01 ) can efficiently mobilize hematopoietic stem cells into peripheral blood, and is a new type of hematopoietic stem cell mobilizing agents. The invention can play an important role in research and development of mobilizing agents for mobilizing hematopoietic stem cells into peripheral blood and has a promising application perspective.
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- Copper-catalyzed C(sp3)-C(sp3) bond formation using a hypervalent iodine reagent: An efficient allylic trifluoromethylation
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An efficient copper-catalyzed allylic trifluoromethylation reaction has been developed. This reaction provides a general and straightforward way to synthesize allylic trifluoromethylated compounds under mild conditions.
- Wang, Xi,Ye, Yuxuan,Zhang, Songnan,Feng, Jiajie,Xu, Yan,Zhang, Yan,Wang, Jianbo
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supporting information; experimental part
p. 16410 - 16413
(2011/11/29)
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- Photoprotection compositions comprising certain chelating agents
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The subject invention relates to methods and compositions comprising: a) from about 0.1% to about 5% of a compound having the structure selected from the group consisting of: STR1 wherein each R is independently selected from the group consisting of hydrogen, alkyl, and aryl; each R' is independently selected from the group consisting of hydrogen, alkoxy, and alkyl; Z and Z' are independently selected from the group consisting of NH, O, and CH2 such that when Z or Z' is NH, the other is not O; or a pharmaceutically acceptable salt of any of the aforementioned compounds; and b) a pharmaceutically-acceptable topical carrier.
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- Complexes of macrocyclic compounds
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Novel macrocyclic (monocyclic and bicyclic) compounds having nitrogen bridgehead atoms and having in the hydrocarbon bridging chains at least two additional hetero atoms selected from the group consisting of sulfur, oxygen, and nitrogen, when admixed with a compatible cation-donor compound form stable cation-containing macrocyclic complexes which, in turn, can be conveniently dissociated by addition of acid or a quaternizing agent. The novel macrocyclics are valuable for use in the same way and for the same purposes as chelating agents.
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- Monocyclic macrocyclic compounds and complexes thereof
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Novel monocyclic macrocyclic compounds having nitrogen bridgehead atoms and having in the hydrocarbon bridging chains at least two additional hetero atoms selected from the group consisting of sulfur, oxygen, and nitrogen, when admixed with a compatible cation-donor compound form stable cation-containing macrocyclic complexes which, in turn, can be conveniently dissociated by addition of acid or a quaternizing agent. The novel macrocyclics are valuable for use in the same way and for the same purposes as chelating agents.
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