Synthesis and Bioactivity of Substituted Benzoylguanidine Derivatives as Potent Na＋/H＋ Exchanger Inhibitors  

作　　者：Jin,Ning Yang,Yun Xu,Wenting Yang,Xiaozhi Gong,Guoqing Xu,Yungen[1] 

机构地区：[1]Department of Medicinal Chemistry,China Pharmaceutical University,Nanjing,Jiangsu 210009,China [2]Department of Pharmacology,China Pharmaceutical University,Nanjing,Jiangsu 210009,China

出　　处：《Chinese Journal of Chemistry》2012年第2期333-340,共8页中国化学（英文版）

基　　金：This work was supported by the National Natural Science Foundation of China （No. 30672512）.

摘　　要：A novel series of substituted benzoylguanidine derivatives were designed and synthesized in order to evaluate their NHE 1 inhibitory activity. Most of them were found to inhibit NHE 1-mediated platelet swelling in a concentration-dependent manner, and eight compounds showed more potent NHE 1 inhibitory activity than Cariporide. Compound 6f with an IC50 value of 1.08 × 10-10 mol·L-1, was 39 times more potent than lead compound CPU-X-050420 in vitro tests.A novel series of substituted benzoylguanidine derivatives were designed and synthesized in order to evaluate their NHE 1 inhibitory activity. Most of them were found to inhibit NHE 1-mediated platelet swelling in a concentration-dependent manner, and eight compounds showed more potent NHE 1 inhibitory activity than Cariporide. Compound 6f with an IC50 value of 1.08 × 10-10 mol·L-1, was 39 times more potent than lead compound CPU-X-050420 in vitro tests.

关 键 词：NHE1 inhibitor benzoylguanidine derivatives ischemia-reperfusion injury 

分 类 号：TQ245.27[化学工程—有机化工] O636.1[理学—高分子化学]