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Design, Synthesis, and Activities of Novel Derivatives of Isophthalamide and Benzene-1,3-disulfonamide
作者姓名:LIU  Xiu-jie  WANG  Song-qing  ZHANG  jing  ZHANG  Feng-xia  LI  Gui-zhu  WANG  Bao-jie  SHAO  Ying-lu  ZHANG  Li-guang  FANG  Lin  CHENG  Mao-sheng
作者单位:LIU Xiu-jie 1,3,WANG Song-qing 2,ZHANG Jing 1,ZHANG Feng-xia 1,LI Gui-zhu 1,WANG Bao-jie 1,SHAO Ying-lu 1,ZHANG Li-guang 1,FANG Lin 1 and CHENG Mao-sheng 11. The College of Pharmaceutical Engineering,Shenyang Pharmaceutical University,Shenyang 110016,P.R. China;2. The College of Pharmaceutical and Biotechnology,Tianjin University,Tianjin 300072,P.R. China;3. The School of Biology and Chemistry,Tianjin University of Technology,Tianjin 300191,P.R. China
摘    要:Introduction Themeritsofantiplatelettherapyforthepreven tionofthrombosisincardiovasculardiseaseareevi dent.Meta analysisresultshaveshownthatsecondary preventionbyantiplateletaggregationagentscanreduce theriskofnonfatalmyocardialinfarction(MI)and strokeby2…

关 键 词:凝血噁烷  抗血小板  合成  活性  异邻苯二酰胺  二磺酰胺  心血管病
文章编号:1005-9040(2006)-03-356-04
收稿时间:2005-03-18

Design, Synthesis, and Activities of Novel Derivatives of Isophthalamide and Benzene-1, 3-disulfonamide
LIU Xiu-jie WANG Song-qing ZHANG jing ZHANG Feng-xia LI Gui-zhu WANG Bao-jie SHAO Ying-lu ZHANG Li-guang FANG Lin CHENG Mao-sheng.Design, Synthesis, and Activities of Novel Derivatives of Isophthalamide and Benzene-1,3-disulfonamide[J].Chemical Research in Chinese University,2006,22(3):356-359.
Authors:Xiu-jie LIU  Song-qing WANG  Jing ZHANG  Feng-xia ZHANG  Gui-zhu LI  Bao-jie WANG  Ying-lu SHAO  Li-guang ZHANG  Lin FANG  Mao-sheng CHENG
Institution:aThe College of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang 110016, P. R. China;bThe College of Pharmaceutical and Biotechnology, Tianjin University, Tianjin 300072, P. R. China;cThe School of Biology and Chemistry, Tianjin University of Technology, Tianjin 300191, P. R. China
Abstract:Based on the antiplatelet aggregation mechanism and the bioisosterism principle of the reference drug picotamide, thirteen novel derivatives of arylamide and arylsulfonamide were designed and prepared. The biological activities of these derivatives were investigated. The chemical structures of the target compounds were confirmed by 1 H NMR and IR. The in vitro activities of antiplatelet aggregation of the thirteen target compounds were assessed by Born's method. Compounds 2b and 8h have significant antiplatelet aggregation activities, which are superior to the corresponding activity of Picotamide.
Keywords:Thromboxane  Antiplatelet  Isophthalamide  Disulfonamide  Synthesis
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