4-Substituted (benzo [b] thiophene-2-carbonyl) guanidines as novel Na+/H+ exchanger isoform-1 (NHE-1) inhibitors

S Lee, H Lee, KY Yi, BH Lee, S Yoo, K Lee…

Index: Lee, Sunkyung; Lee, Hyunsuk; Kyu, Yang Yi; Byung, Ho Lee; Yoo, Sung-Eun; Lee, Kyunghee; Nam, Sook Cho Bioorganic and Medicinal Chemistry Letters, 2005 , vol. 15, # 12 p. 2998 - 3001

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Citation Number: 18

Abstract

A series of 4-substituted (benzo [b] thiophene-2-carbonyl) guanidines was synthesized and evaluated for the NHE-1 inhibitory activity and cardioprotective efficacy both in vitro and in vivo. Several analogs exhibited a strong inhibition on NHE-1, and which was generally well correlated with their cardioprotective efficacy. Especially the 4-nitro 20 and cyano 50 compounds excellently improved the cardiac function and reduced infarct size against ...