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

高等学校化学研究 ›› 2006, Vol. 22 ›› Issue (3): 356-359.

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

LIU Xiu-jie^1,3, WANG Song-qing², ZHANG Jing¹, ZHANG Feng-xia¹, LI Gui-zhu¹, WANG Bao-jie¹, SHAO Ying-lu¹, ZHANG Li-guang¹, FANG Lin¹, CHENG Mao-sheng¹

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

收稿日期:2005-03-18 出版日期:2006-06-24 发布日期:2011-08-06

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

LIU Xiu-jie^1,3, WANG Song-qing², ZHANG Jing¹, ZHANG Feng-xia¹, LI Gui-zhu¹, WANG Bao-jie¹, SHAO Ying-lu¹, ZHANG Li-guang¹, FANG Lin¹, CHENG Mao-sheng¹

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

Received:2005-03-18 Online:2006-06-24 Published:2011-08-06

摘要/Abstract

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 Born'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

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 ¹H 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.

Key words: Thromboxane, Antiplatelet, Isophthalamide, Disulfonamide, Synthesis

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]. 高等学校化学研究, 2006, 22(3): 356-359.

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

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

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