Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 22, Issue 5, Pages 2052-2062Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2012.01.015
Keywords
Na(v)1.7; Voltage-gated sodium channels; Na-v channels; Sodium channel blockers; Sodium channel inhibitors; Sodium channel antagonists; Congenital indifference to pain; Paroxysmal extreme pain disorder; Primary erythromelalgia; Pyrrolopyrimidine
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Herein we describe the discovery, optimization, and structure-activity relationships of novel potent pyrrolopyrimidine Na(v)1.7 antagonists. Hit-to-lead SAR studies of the pyrrolopyrimidine core, head, and tail groups of the molecule led to the identification of pyrrolopyrimidine 48 as exceptionally potent Na(v)1.7 blocker with good selectivity over hERG and improved microsomal stability relative to our hit molecule and pyrazolopyrimidine 8 as a promising starting point for future optimization efforts. Published by Elsevier Ltd.
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