Dihydropyrazolopyrimidine inhibitors of K(V)1.5 (I(Kur))

Wayne Vaccaro; Tram Huynh; John Lloyd; Karnail Atwal; Heather J Finlay; Paul Levesque; Mary Lee Conder; Tonya Jenkins-West; Hong Shi; Lucy Sun

doi:10.1016/j.bmcl.2008.10.099

Dihydropyrazolopyrimidine inhibitors of K(V)1.5 (I(Kur))

Bioorg Med Chem Lett. 2008 Dec 15;18(24):6381-5. doi: 10.1016/j.bmcl.2008.10.099. Epub 2008 Oct 25.

Authors

Wayne Vaccaro¹, Tram Huynh, John Lloyd, Karnail Atwal, Heather J Finlay, Paul Levesque, Mary Lee Conder, Tonya Jenkins-West, Hong Shi, Lucy Sun

Affiliation

¹ Bristol-Myers Squibb, Route 206 & Provinceline Road, PO Box 4000, Princeton, NJ 08543-4000, USA. wayne.vaccaro@bms.com

PMID: 19004630
DOI: 10.1016/j.bmcl.2008.10.099

Abstract

A series of dihydropyrazolopyrimidine inhibitors of K(V)1.5 (I(Kur)) have been identified. The synthesis, structure-activity relationships and selectivity against several other ion channels are described.

MeSH terms

Animals
Atrial Fibrillation / metabolism
Cell Line
Chemistry, Pharmaceutical / methods*
Drug Design
Humans
Ions / chemistry
Mice
Models, Chemical
Potassium Channel Blockers / chemical synthesis*
Potassium Channel Blockers / pharmacology
Potassium Channels, Voltage-Gated / antagonists & inhibitors*
Pyrimidines / chemical synthesis*
Pyrimidines / pharmacology*
Stereoisomerism
Structure-Activity Relationship

Substances

Ions
Potassium Channel Blockers
Potassium Channels, Voltage-Gated
Pyrimidines