期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 22, 期 5, 页码 2033-2042出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2012.01.023
关键词
Na(v)1.7; Analgesia; Sodium channels; Aminopyrazine
Herein the discovery of a novel class of aminoheterocyclic Na(v)1.7 antagonists is reported. Hit compound 1 was potent but suffered from poor pharmacokinetics and selectivity. The compact structure of 1 offered a modular synthetic strategy towards a broad structure-activity relationship analysis. This analysis led to the identification of aminopyrazine 41, which had vastly improved hERG selectivity and pharmacokinetic properties. (C) 2012 Elsevier Ltd. All rights reserved.
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