201003-31-8Relevant academic research and scientific papers
Nature-inspired pyrrolo[2,3-d]pyrimidines targeting the histamine H3 receptor
Frank, Annika,Meza-Arriagada, Francisco,Salas, Cristian O.,Espinosa-Bustos, Christian,Stark, Holger
, p. 3194 - 3200 (2019)
Inspired by marine compounds the derivatization of the natural pyrrolo[2,3-d]pyrimidine lead scaffold led to a series of novel compounds targeting the histamine H3 receptor. The focus was set on improved binding towards the receptor and to esta
Discovery and hit-to-lead optimization of pyrrolopyrimidines as potent, state-dependent Nav1.7 antagonists
Chakka, Nagasree,Bregman, Howie,Du, Bingfan,Nguyen, Hanh Nho,Buchanan, John L.,Feric, Elma,Ligutti, Joseph,Liu, Dong,McDermott, Jeff S.,Zou, Anruo,McDonough, Stefan I.,Dimauro, Erin F.
scheme or table, p. 2052 - 2062 (2012/04/17)
Herein we describe the discovery, optimization, and structure-activity relationships of novel potent pyrrolopyrimidine Nav1.7 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 Nav1.7 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.
