Design, Synthesis, and Activities of Novel Derivativesof Isophthalamide and Benzene-1,3-disulfonamide  

作　　者：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 

机构地区：[1]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

出　　处：《Chemical Research in Chinese Universities》2006年第3期356-359,共4页高等学校化学研究（英文版）

摘　　要：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 ^1H NMR and IR. The in vitro activities of antiplatelet aggregation of the thirteen target compounds were assessed by Bore＇s method. Compounds 2b and 8h have significant antiplatelet aggregation activities, which are superior to the corresponding activity of Picotamide.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 ^1H NMR and IR. The in vitro activities of antiplatelet aggregation of the thirteen target compounds were assessed by Bore＇s method. Compounds 2b and 8h have significant antiplatelet aggregation activities, which are superior to the corresponding activity of Picotamide.

关 键 词：THROMBOXANE ANTIPLATELET Isophthalamide Disulfonamide SYNTHESIS 

分 类 号：R972[医药卫生—药品] R914[医药卫生—药学]