Referenced in: none

Automatically associated channels: TRP , TRPV , TRPV1

Title: Discovery and synthesis of 6,7,8,9-tetrahydro-5H-pyrimido-[4,5-d]azepines as novel TRPV1 antagonists.

Authors: Natalie A Hawryluk, Jeffrey E Merit, Alec D Lebsack, Bryan J Branstetter, Michael D Hack, Nadia Swanson, Hong Ao, Michael P Maher, Anindya Bhattacharya, Qi Wang, Jamie M Freedman, Brian P Scott, Alan D Wickenden, Sandra R Chaplan, J Guy Breitenbucher

Journal, date & volume: Bioorg. Med. Chem. Lett., 2010 Dec 1 , 20, 7137-41

PubMed link: http://www.ncbi.nlm.nih.gov/pubmed/20947352

Abstract
Utilization of a tetrahydro-pyrimdoazepine core as a bioisosteric replacement for a piperazine-urea resulted in the discovery a novel series of potent antagonists of TRPV1. The tetrahydro-pyrimdoazepines have been identified as having good in vitro and in vivo potency and acceptable physical properties.