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Bioorg Med Chem Lett. 2013 Mar 15;23(6):1743-7. doi: 10.1016/j.bmcl.2013.01.064. Epub 2013 Jan 26.

Triazolo and imidazo dihydropyrazolopyrimidine potassium channel antagonists.

Author information

1
Department of Discovery Chemistry, Bristol-Myers Squibb, Research and Development, PO Box 5400, Princeton, NJ 08543-5400, United States. heather.finlay@bms.com

Abstract

Previously disclosed C6 amido and benzimidazole dihydropyrazolopyrimidines were potent and selective blockers of IKur current. Syntheses and SAR for C6 triazolo and imidazo dihydropyrazolopyrimidines series are described. Trifluoromethylcyclohexyl N(1) triazole, compound 51, was identified as a potent and selective Kv1.5 inhibitor with an acceptable PK and liability profile.

PMID:
23414837
DOI:
10.1016/j.bmcl.2013.01.064
[Indexed for MEDLINE]

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