Bioorganic & Medicinal Chemistry Letters 2013-03-15

Triazolo and imidazo dihydropyrazolopyrimidine potassium channel antagonists.

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

Index: Bioorg. Med. Chem. Lett. 23(6) , 1743-7, (2013)

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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.Copyright © 2013 Elsevier Ltd. All rights reserved.