Referenced in: none

Automatically associated channels: Kv1.5

Title: Triazolo and imidazo dihydropyrazolopyrimidine potassium channel antagonists.

Authors: Heather J Finlay, Ji Jiang, Yolanda Caringal, Alexander Kover, Mary Lee Conder, Dezhi Xing, Paul Levesque, Timothy Harper, Mei Mann Hsueh, Karnail Atwal, Michael Blanar, Ruth Wexler, John Lloyd

Journal, date & volume: Bioorg. Med. Chem. Lett., 2013 Mar 15 , 23, 1743-7

PubMed link: http://www.ncbi.nlm.nih.gov/pubmed/23414837

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.