1366234-32-3Relevant articles and documents
The discovery of aminopyrazines as novel, potent Nav1.7 antagonists: Hit-to-lead identification and SAR
Bregman, Howard,Nguyen, Hanh Nho,Feric, Elma,Ligutti, Joseph,Liu, Dong,McDermott, Jeff S.,Wilenkin, Ben,Zou, Anruo,Huang, Liyue,Li, Xingwen,McDonough, Stefan I.,Dimauro, Erin F.
, p. 2033 - 2042 (2012)
Herein the discovery of a novel class of aminoheterocyclic Na v1.7 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.
