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.
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Triazolo and imidazo dihydropyrazolopyrimidine potassium channel antagonists.
Bioorg Med Chem Lett
March 2013
Department of Discovery Chemistry, Bristol-Myers Squibb, Research and Development, PO Box 5400, Princeton, NJ 08543-5400, United States.
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.
View Article and Find Full Text PDFDihydropyrazolopyrimidines containing benzimidazoles as K(V)1.5 potassium channel antagonists.
Bioorg Med Chem Lett
September 2009
Bristol-Myers Squibb, Pharmaceutical Research and Development, PO Box 5400, Princeton, NJ 08543-5400, USA.
Dihydropyrazolopyrimidines with a C6 heterocycle substituent were found to have high potency for block of K(V)1.5. Investigation of the substitution in the benzimidazole ring and the substituent in the 5-position of the dihydropyrazolopyrimidine ring produced 31a with an IC50 for K(V)1.
View Article and Find Full Text PDFDihydropyrazolopyrimidine inhibitors of K(V)1.5 (I(Kur)).
Bioorg Med Chem Lett
December 2008
Bristol-Myers Squibb, Route 206 & Provinceline Road, PO Box 4000, Princeton, NJ 08543-4000, USA.
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.
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