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

2010; Elsevier BV; Volume: 20; Issue: 23 Linguagem: Inglês

10.1016/j.bmcl.2010.09.023

1464-3405

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 Freedman, Brian Scott, Alan D. Wickenden, Sandra R. Chaplan, J. Guy Breitenbucher,

Herbal Medicine Research Studies

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.