N-Aryl azacycles as novel sodium channel blockers.

Stephen M Lynch,Laykea Tafesse,Kevin Carlin,Parijat Ghatak,Bin Shao,Haissam Abdelhamid,Donald J Kyle

Bioorganic & Medicinal Chemistry Letters（2015）

引用 12|浏览5

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摘要

We have identified a new series of N-aryl azacycles as sodium channel blockers, which showed good potency on Na(v)1.7 in FLIPR-based and electrophysiological functional assays. Analogs from this series possessed selectivity over hERG, reasonable oral exposure in rat PK studies and are predicted to have limited CNS penetration. (C) 2014 Elsevier Ltd. All rights reserved.

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ARXQEUXKXBDCRA-JJRNEHELSA-N,XJOGDSABVMVHKS-UHFFFAOYSA-N,GAFPQLZAICTDSD-MZGUNHGESA-N

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