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

Autor:	Qi Wang, J. Guy Breitenbucher, Hong Ao, Michael D. Hack, Bryan James Branstetter, Alan D. Wickenden, Jamie M. Freedman, Alec D. Lebsack, Nadia Swanson, Michael P. Maher, Sandra R. Chaplan, Natalie A. Hawryluk, Jeffrey E. Merit, Brian Scott, Anindya Bhattacharya
Rok vydání:	2010
Předmět:	Chemistry Stereochemistry organic chemicals Organic Chemistry Clinical Biochemistry TRPV1 TRPV Cation Channels Pharmaceutical Science Azepines Biochemistry Chemical synthesis In vitro Rats Structure-Activity Relationship In vivo Drug Discovery polycyclic compounds Animals Molecular Medicine Potency heterocyclic compounds Molecular Biology
Zdroj:	Bioorganic & Medicinal Chemistry Letters. 20:7137-7141
ISSN:	0960-894X
DOI:	10.1016/j.bmcl.2010.09.023
Popis:	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.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::577da627a65a624579ac5616942548f2 https://doi.org/10.1016/j.bmcl.2010.09.023 Zobrazit plný text záznamu Full Text from ScienceDirect