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Synthesis and Biological Evaluation of 1-Heteroarylmethyl 1,4-Diazepanes Derivatives as Potential T-type Calcium Channel Blockers

Authors: Ullapu, Punna Reddy; Ku, Su Jin; Choi, Yeon Hee; Park, Jiyeon; Han, So-Yeop; Baek, Du Jong; Lee, Jaekyun; Pae, Ae Nim; Min, Sun-Joon; Cho, Yong Seo

Issue Date: 2011-08-20

Publisher: KOREAN CHEMICAL SOC

Citation: BULLETIN OF THE KOREAN CHEMICAL SOCIETY, v.32, no.8, pp.3063 - 3073

Abstract: The synthesis and biological evaluation of 1-heteroarylmethyl 1,4-diazepane derivatives as potential T-type calcium channel blockers is described. In this study, we have identified the compound 211 exhibiting the most potent T-type calcium channel blocking activity with IC(50) value of 0.20 mu M, which is superior to that of mibefradil.

Keywords: CA2+ CHANNELS; ANTAGONISTS; INHIBITION; ACID; CA2+ CHANNELS; ANTAGONISTS; INHIBITION; ACID; T-type calcium channel blockers; 1,4-Diazepanes; Heteroaromatic compounds; FDSS6000 assay; Patch-clamp assay

ISSN: 0253-2964

URI: https://pubs.kist.re.kr/handle/201004/130071

DOI: 10.5012/bkcs.2011.32.8.3063

Appears in Collections:: KIST Article > 2011

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