Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10593800 | Bioorganic & Medicinal Chemistry Letters | 2012 | 10 Pages |
Abstract
Herein the discovery of a novel class of aminoheterocyclic Nav1.7 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.
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Authors
Howard Bregman, Hanh Nho Nguyen, Elma Feric, Joseph Ligutti, Dong Liu, Jeff S. McDermott, Ben Wilenkin, Anruo Zou, Liyue Huang, Xingwen Li, Stefan I. McDonough, Erin F. DiMauro,