4.5 Article

Pyridyl amides as potent inhibitors of T-type calcium channels

期刊

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 21, 期 6, 页码 1692-1696

出版社

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2011.01.089

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T-type calcium channel; Structure-activity relationships; Pregnane X receptor; Electrocorticogram; Epilepsy

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A novel series of amide T-type calcium channel antagonists were prepared and evaluated using in vitro and in vivo assays. Optimization of the screening hit 3 led to identification of the potent and selective T-type antagonist 37 that displayed in vivo efficacy in rodent models of epilepsy and sleep. (C) 2011 Elsevier Ltd. All rights reserved.

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