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Synthesis and biological evaluation of 1,4-diazepane derivatives as T-type calcium channel blockers

Authors: Gu, Su Jin; Lee, Jae Kyun; Pae, Ae Nim; Chung, Hye Jin; Rhim, Hyewon; Han, So Yeob; Min, Sun-Joon; Cho, Yong Seo

Citation: Bioorganic & Medicinal Chemistry Letters, v.20, no.9, pp.2705 - 2708

Abstract: We have synthesized and biologically evaluated 1,4-diazepane derivatives as T-type calcium channel blockers. In this study, we discovered compound 4s, a potential T-type calcium channel blocker with good selectivity over hERG and N-type calcium channels. In addition, it exhibited favorable pharmacokinetic characteristics for further investigation of T-type calcium channel related diseases. (C) 2010 Elsevier Ltd. All rights reserved.

Keywords: CA2+ CHANNELS; DESIGN; ANTAGONISTS; MIBEFRADIL; DISCOVERY; CA2+ CHANNELS; DESIGN; ANTAGONISTS; MIBEFRADIL; DISCOVERY; T-type calcium channel blockers; 1,4-Diazepane; Pharmacokinetics

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