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

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 propert...

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Bibliographic Details
Published inBioorganic & medicinal chemistry letters Vol. 20; no. 23; pp. 7137 - 7141
Main Authors Hawryluk, Natalie A., Merit, Jeffrey E., Lebsack, Alec D., Branstetter, Bryan J., Hack, Michael D., Swanson, Nadia, Ao, Hong, Maher, Michael P., Bhattacharya, Anindya, Wang, Qi, Freedman, Jamie M., Scott, Brian P., Wickenden, Alan D., Chaplan, Sandra R., Breitenbucher, J. Guy
Format Journal Article
LanguageEnglish
Published Elsevier Ltd 2010
Subjects
Tetrahydro-pyrimdoazepine
TRPV1
Vanilloid
Vanilloid
TRPV1
Tetrahydro-pyrimdoazepine
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Summary: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.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2010.09.023