Discovery of benzamide derivatives as potent Kv1.5 inhibitors

doi:10.5246/jcps.2012.06.070

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Discovery of benzamide derivatives as potent Kv1.5 inhibitors

Xiaoke Guo, Zheng Shen, Peng Yu, Hongxi Chu, Yiqun Tang, Qidong You*

1. Jiangsu Key Laboratory of Drug Design and Optimization, China Pharmaceutical University, Nanjing 210009, China
2. Research Division of Pharmacology, China Pharmaceutical University, Nanjing 210009, China

Received:2012-06-14 Revised:2012-08-20 Online:2012-10-25 Published:2012-10-25
Contact: Qidong You*

Abstract

Abstract: Kv1.5 potassium channel is reported as a potent and safe target for atrial fibrillation. CPUY11018 was proved it had moderate inhibition of Kv1.5. In order to improve the stability of CPUY11018, and investigate the structure-activity relationship, 4 series of benzamide derivatives were synthesized and evaluated. Among them, 8c is a most potent inhibitor of Kv1.5.

Key words: Kv1.5, Ultra-rapid potassium current, Potassium channel, Atrial fibrillation

CLC Number:

R916

Supporting:

Xiaoke Guo, Zheng Shen, Peng Yu, Hongxi Chu, Yiqun Tang, Qidong You* . Discovery of benzamide derivatives as potent Kv1.5 inhibitors [J]. , DOI: 10.5246/jcps.2012.06.070.

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Discovery of benzamide derivatives as potent Kv1.5 inhibitors

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