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 Jan 1

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We have identified a new series of N-aryl azacycles as sodium channel blockers, which showed good potency on Nav1.7 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. Copyright © 2014 Elsevier Ltd. All rights reserved.

Citation

Stephen M Lynch, Laykea Tafesse, Kevin Carlin, Parijat Ghatak, Bin Shao, Haissam Abdelhamid, Donald J Kyle. N-Aryl azacycles as novel sodium channel blockers. Bioorganic & medicinal chemistry letters. 2015 Jan 1;25(1):48-52