期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 16, 期 22, 页码 5859-5863出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2006.08.057
关键词
semicarbazone; Kv1.5 inhibitor; atrial antiarrhythmic; in-vivo efficacy
A novel class of tetrahydroindolone-derived semicarbazones has been discovered as potent Kv 1.5 blockers. in in vitro studies, several compounds exhibited very good potency for blockade of Kv 1.5. Compound 8i showed good selectivity for blockade of Kv1.5 vs hERG and L-type calcium channels. In an anesthetized pig model, compounds 8i and 10c increased atrial ERP about 28%, 18%, respectively, in the right atrium without affecting ventricular ERP. (c) 2006 Elsevier Ltd. All rights reserved.
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