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Synthesis and in vitro-Anti-hepatitis B Virus Activities of Several Ethyl 5-Hydroxy-1H-indole-3-carboxylates 被引量:16
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作者 ZHAO Chun-shen ZHAO Yan-fang CHAI Hui-fang GONG Ping 《Chemical Research in Chinese Universities》 SCIE CAS CSCD 2006年第5期577-583,共7页
A series of ethyl 5-hydroxyindole-3-earboxylates 6a-10r was designed and synthesized. The structures of all the compounds were confirmed by IR, ^1H NMR, and MS and their anti-hepatitis B virus (HBV) activities were ... A series of ethyl 5-hydroxyindole-3-earboxylates 6a-10r was designed and synthesized. The structures of all the compounds were confirmed by IR, ^1H NMR, and MS and their anti-hepatitis B virus (HBV) activities were evaluated in 2.2.15 cells. Among them, compound 7g { ethyl 5-hydroxy-2- [ ( 3-methoxyphenylsulfinyl ) methyl ] -1-methyl-4- [ (4-methylpiperazin-1-yl) methyl ]-1H-indole-3-carboxylate} displays a significant anti-HBV activity, which is more potent than the positive control lamivudine. 展开更多
关键词 Ethyl 5-hydroxy-1h-indole-3-carboxylates SYNTHESIS Anti-hepatitis B virus activity
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Synthesis and in vitro Anti-hepatitis B Virus Activity of Some Ethyl 5-Hydroxy-4-substituted Aminomethyl-2-sulfinylmethyl-1H-indole-3-carboxylates
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作者 ZHAO Yah-fang FENG Run-liang +2 位作者 LIU Ya-jing ZHANG Yi-kun GONG Ping 《Chemical Research in Chinese Universities》 SCIE CAS CSCD 2010年第2期272-277,共6页
A novel series of ethyl 5-hydroxy-4-substituted aminomethyl-2-sulfinylmethyl-lH-indole-3-carboxylates 8a--8j and 11e--11f was synthesized and evaluated in HepG2.2.15 cells for their anti-hepatitits B virus(HBV) acti... A novel series of ethyl 5-hydroxy-4-substituted aminomethyl-2-sulfinylmethyl-lH-indole-3-carboxylates 8a--8j and 11e--11f was synthesized and evaluated in HepG2.2.15 cells for their anti-hepatitits B virus(HBV) activity and cytotoxicity. Among them, six compounds showed more potent inhibitory activity than lamivudine. Compound 8e exhibited the most significant anti-HBV activity with an IC50 value of 1.62 μmol/L, which was 33-times more potent than the reference drug lamivudine(IC50=54.78μmol/L). 展开更多
关键词 5-Hydroxy-2-sulfinylmethyl-1h-indole-3-carboxylates Anti-hepatitis B virus activity SYNTHESIS
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Synthesis and Crystal Structure of 3-(1-Ethyl-1H-indole-3-carbonyl)aminopropionic Acid
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作者 黄岗 徐兴烟 +1 位作者 曾向潮 李凯平 《Chinese Journal of Structural Chemistry》 SCIE CAS CSCD 2010年第9期1343-1346,共4页
3-(1-Ethyl-1H-indole-3-carbonyl)aminopropionic acid has been synthesized by alkylation of 3-(1H-indole-3-carbonyl)aminopropionic acid methyl ester with bromoethane,follo-wed by saponifying and acidating,in 89.0% y... 3-(1-Ethyl-1H-indole-3-carbonyl)aminopropionic acid has been synthesized by alkylation of 3-(1H-indole-3-carbonyl)aminopropionic acid methyl ester with bromoethane,follo-wed by saponifying and acidating,in 89.0% yield.Its crystal structure was gotten and determined by X-ray diffraction method.The crystal is of orthorhombic,space group P212121 with a = 8.9490(12),b = 11.1010(15),c = 13.0475(18) ,V = 1296.2(3) 3,Z = 4,Dc = 1.334 g/cm3,λ = 0.71073 ,μ(MoKα) = 0.095 mm-1,Mr = 260.29 and F(000) = 552.The structure was refined to R = 0.0306 and wR = 0.1445 for 2612 observed reflections with I 2σ(I).In the crystal structure,molecules are linked to each other through hydrogen bonds of N(2)-H(2)···O(1) and O(3)-H(3)···O(1),generating a three-dimensional network. 展开更多
关键词 3-(1-ethyl-1h-indole-3-carbonyl)aminopropionic acid INDOLE synthesis crystal structure
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Drug discovery based on the structure of FKBP12: Design, synthesis and evaluation of L-1,4-thiazane-3-carboxylic acid derivatives as neuroimmunophilin ligands
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作者 NIE AiHua XIAO JunHai +4 位作者 WANG LiLi LIAO GuoChao LIU HongYing REN Shen LI Song 《Science China Chemistry》 SCIE EI CAS 2007年第3期405-417,共13页
By choosing neuroimmunophilin FKBP12 as a therapeutical target, we have attempted to discover a new structural drug for treating neurodegenerative disease. This drug should possess neurotrophic activity and not affect... By choosing neuroimmunophilin FKBP12 as a therapeutical target, we have attempted to discover a new structural drug for treating neurodegenerative disease. This drug should possess neurotrophic activity and not affect the immune system. Based on the crystal structure of FKBP12, FK506 and Calcineurin complex, a series of small organic molecules were designed. These molecules were to have the ability of binding to FKBP12 in a virtual screening. By using a solution parallel synthetic method, these compounds were synthesized. The neuroprotective and neuroregenerative activities of these compounds were evaluated by binding assays, PC12 cells survival and neurite outgrowth model, chick dorsal root ganglion cultures (DRG) and 6-OHDA lesioned mice sympathetic nerve endings model. The evaluation results of these compounds showed that compound N308 has great promise as a candidate for a neuroprotective and neuroregenerative agent. 展开更多
关键词 FKBP12 L-1 4-thiazane-3-carboxylic acid derivatives DESIGN SYNTHESIS NEUROTROPHIC activity
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Hydrothermal Synthesis and Crystal Structure of One Novel 1-D Copper(Ⅱ)-organic Framework:{[Cu_2(PP)_2(CBPC)]_2·7H_2O}_n 被引量:2
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作者 魏培海 吴小园 +5 位作者 范黎明 李大成 张修堂 窦建民 刘新征 石聪文 《Chinese Journal of Structural Chemistry》 SCIE CAS CSCD 2010年第12期1774-1779,共6页
One novel 1-D copper(Ⅱ)-organic compound,namely {[Cu2(PP)2(CBPC)]2·7H2O}n(1,H2CBPC=1-[(2'-carboxybiphenyl-4-yl)methyl]-2-propylimidazole-4-carboxylic acid,HPP=3-(2-pyridyl)pyrazole),was synthesized ... One novel 1-D copper(Ⅱ)-organic compound,namely {[Cu2(PP)2(CBPC)]2·7H2O}n(1,H2CBPC=1-[(2'-carboxybiphenyl-4-yl)methyl]-2-propylimidazole-4-carboxylic acid,HPP=3-(2-pyridyl)pyrazole),was synthesized under hydrothermal conditions.X-ray diffraction analyses reveal that the two Cu(Ⅱ) ions in the distorted dimer [Cu2(PP)2] of 1 are linked by the carboxylate oxygen atoms on the phenyl and imidazole rings,respectively,forming one interesting snake-like chain.Single-crystal X-ray analyses reveal that it crystallizes in monoclinic,space group C2/c with a=30.656(8),b=12.715(3),c=22.405(5),β=122.758(3)°,V=7344(3)3,Z=4,Mr=1681.65,Dc=1.521 g/cm3,F(000)=3464,μ=1.221 mm-1,the final R=0.0453 and wR=0.1023 for 4617 observed reflections with Ⅰ 〉2σ(Ⅰ). 展开更多
关键词 1-[(2'-carboxybiphenyl-4-yl)methyl]-2-propylimidazole-4-carboxylic acid 3-(2-pyridyl)pyrazole) copper(Ⅱ) TGA XPS crystal structures
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Synthesis,Characterization and Structure of Chiral Amino Acids and Their Corresponding Amino Alcohols with Camphoric Backbone
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作者 QIAN Hui-Fen HUANG Wei +1 位作者 LI Hui-Hui YAO Cheng 《Chinese Journal of Structural Chemistry》 SCIE CAS CSCD 北大核心 2006年第10期1243-1249,共7页
Chiral amino acids and their corresponding amino alcohols bearing camphoric backbone were prepared from D-(+)-camphoric imide and characterized by infrared, elemental analysis, ESI-MS, and NMR measurements. Among t... Chiral amino acids and their corresponding amino alcohols bearing camphoric backbone were prepared from D-(+)-camphoric imide and characterized by infrared, elemental analysis, ESI-MS, and NMR measurements. Among them, one intermediate (1S,3R)-3-amino-2,2,3- trimethyl cyclopentane-1-carboxylic acid hydrochloride 3 was structurally elucidated by X-ray diffraction techniques. Versatile intermolecular hydrogen bonding interactions observed in its packing structure result in a two-dimensional framework. 展开更多
关键词 chiral amino acids and amino alcohols 1S 3R)-3-amino-2 2 3-trimethyl-cyclopentane-1-carboxylic acid hydrochloride hydrogen-bonding interactions crystal structures
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Synthesis,Structure,and Magnetic Property of One Snake-shaped Copper(Ⅱ)-organic Compound:Cu[Cu_2(PP)_2](CBPC)_2]·2(H_2O) 被引量:3
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作者 范黎明 李大成 +2 位作者 魏培海 张修堂 窦建民 《Chinese Journal of Structural Chemistry》 SCIE CAS CSCD 2011年第10期1381-1386,共6页
One novel copper(II)-organic compound,namely Cu[Cu2(PP)2](CBPC)2]·2(H2O)(1,H2CBPC = 1-[(2'-carboxybiphenyl-4-yl)methyl]-2-propylimidazole-4-carboxylic acid,HPP = 3-(2-pyridyl)pyrazole),was designed... One novel copper(II)-organic compound,namely Cu[Cu2(PP)2](CBPC)2]·2(H2O)(1,H2CBPC = 1-[(2'-carboxybiphenyl-4-yl)methyl]-2-propylimidazole-4-carboxylic acid,HPP = 3-(2-pyridyl)pyrazole),was designed and synthesized under hydrothermal conditions.X-ray diffraction analysis reveals that two Cu(II)ions in the quasi-planar dimmer of [Cu2(PP)2] are linked by the carboxylate oxygen atoms on the phenyl ring and the imidazole ring,respectively,yielding one snake-shaped structure.Magnetic measurements reveal that compound 1 shows the strongly antiferromagnetic property.Crystal data of 1:C58H52Cu3N10O10,Mr = 1239.72,monoclinic,P21/c,a = 14.900(7),b = 15.029(7),c = 12.308(6),β = 102.519(9)o,V = 2691(2)3,Z = 2,Dc = 1.530 g/cm3,F(000)= 1274,μ = 1.246 mm-1,R = 0.0416,wR = 0.0780(I 2σ(I))and S = 0.999. 展开更多
关键词 1-[(2'-carboxybiphenyl-4-yl)methyl]-2-propylimidazole-4-carboxylic acid 3-(2-pyridyl)pyrazole) copper(II) magnetism TGA XPS
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The Dependence of <i>N</i>-Malonyltryptophan Formation in Plants on Water Deficit (Review)
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作者 Kim Z. Gamburg 《Natural Science》 2021年第2期26-41,共16页
Drought stress in plants is accompanied by several metabolic changes. One of them is the appearance of <em>N</em>-malonyltryptophan (MT) during leaf wilting of many species, but there is a significant numb... Drought stress in plants is accompanied by several metabolic changes. One of them is the appearance of <em>N</em>-malonyltryptophan (MT) during leaf wilting of many species, but there is a significant number of plant species in which the appearance of MT did not occur. Plants of some species were able to synthesize also <em>N</em>-acetyltryptophan (AT). Excised tomato leaves incubated with D-amino acids (including D-Trp) transform them into malonyl- and acetyl-derivatives even without water deficit. However, MT which appeared during water deficit has been shown to contain L-Trp. Amino acid—1-amino-cyclopropane-1-carboxylic acid (ACC) is also malonylated during water deficit, but other L-amino acids were not malonylated. <em>N</em>-malonyl transferases specific for Trp and ACC have been found in several plants. The existence of <em>N</em>-malonyltransferase specific to L-Trp and appeared during water deficit in plants forming MT is supposed, but clear experimental proof has not been obtained yet. Plants can transform MT applied exogenously into Trp and further to indole-3-acetic acid (IAA). But no evidence has been appeared up to now that endogenous MT may be a source of IAA. It is unknown till now why it is necessary for plants of many species to malonylate only Trp during water deficit. How MT metabolized in animals and if it affects them is also unknown. The necessity to use molecular-genetic approaches for the elucidation of the physiological significance of MT formation during water deficit is underlined. 展开更多
关键词 Drought Stress N-Acetyltryptophan 1-Aminocyclopropane-1-carboxylic acid Indole-3-Acetic acid Tryptophan Malonylation
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Three pairs of alkaloid enantiomers from the root of Isatis indigotica 被引量:12
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作者 Yufeng Liu Xiaoliang Wang +3 位作者 Minghua Chen Sheng Lin Li Li Jiangong Shi 《Acta Pharmaceutica Sinica B》 SCIE CAS CSCD 2016年第2期141-147,188,共8页
Three pairs of enantiomerically pure alkaloids with diverse structure features, named isatindigoticoic acid A and epiisatindigoticoic acid A [(—)-1 and(+)-1], phaitanthrin A and epiphaitanthrin A [(—)-2 and(+)-2], a... Three pairs of enantiomerically pure alkaloids with diverse structure features, named isatindigoticoic acid A and epiisatindigoticoic acid A [(—)-1 and(+)-1], phaitanthrin A and epiphaitanthrin A [(—)-2 and(+)-2], and isatindopyrromizol A and epiisatindopyrromizol A [(—)-3and(+)-3], respectively, were isolated from an aqueous extract of the roots of Isatis indigotica. Racemic and scalemic mixtures of these enantiomers were separated by HPLC on a chiral semi-preparative column.Their structures including absolute configurations were determined by extensive spectroscopic analysis in conjunction with the calculation of electronic circular dichroism(ECD) spectra. The enantiomer pairs possess parent structures of 2-oxo-1,2,3,4-tetrahydroquinoline-4-carboxylic acid, indolo[2,1-b]quinazolinone, and 3-thioxohexahydro-1H-pyrrolo[1,2-c]imidazol-1-one, respectively. Except for phaitanthrin A[(—)-2] which the configuration was previously undetermined, these compounds are new enantiomeric natural products. 展开更多
关键词 CRUCIFERAE Isatis indigotica ALKALOID ENANTIOMER Chiral separation 2-Oxo-1 2 3 4-tetrahydroquinoline-4-carboxylic acid Indolo[2 1-b]quinazolinone 3-Thioxohexahydro-1H-pyrrolo[1 2-c]imidazol-1-one
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