- Discovery and synthesis of 6,7,8,9-tetrahydro-5H-pyrimido-[4,5-d]azepines as novel TRPV1 antagonists.
Discovery and synthesis of 6,7,8,9-tetrahydro-5H-pyrimido-[4,5-d]azepines as novel TRPV1 antagonists.
Bioorganic & medicinal chemistry letters (2010-10-16)
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
PMID20947352
摘要
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.