Triazolo and imidazo dihydropyrazolopyrimidine potassium channel antagonists

…, J Jiang, Y Caringal, A Kover, ML Conder…

Index: Finlay, Heather J.; Jiang, Ji; Caringal, Yolanda; Kover, Alexander; Conder, Mary Lee; Xing, Dezhi; Levesque, Paul; Harper, Timothy; Hsueh, Mei Mann; Atwal, Karnail; Blanar, Michael; Wexler, Ruth; Lloyd, John Bioorganic and Medicinal Chemistry Letters, 2013 , vol. 23, # 6 p. 1743 - 1747

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Citation Number: 3

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.