Dihydropyrazolopyrimidines containing benzimidazoles as KV1.5 potassium channel antagonists
作者： John Lloyd , Heather J. Finlay , Karnail Atwal , Alexander Kover , Joseph Prol
DOI: 10.1016/J.BMCL.2009.07.083
关键词: Substituent 、 Stereochemistry 、 Ion channel 、 Benzimidazole 、 Structure–activity relationship 、 Ring (chemistry) 、 Potency 、 Bioavailability 、 Chemistry 、 Voltage-gated potassium channel 、 Organic chemistry 、 Clinical biochemistry 、 Molecular medicine 、 Biochemistry 、 Molecular biology 、 Drug discovery 、 Pharmaceutical Science
摘要: Dihydropyrazolopyrimidines with a C6 heterocycle substituent were found to have high potency for block of K(V)1.5. Investigation the substitution in benzimidazole ring and 5-position dihydropyrazolopyrimidine produced 31a an IC50 K(V)1.5 0.030muM without significant other cardiac ion channels. This compound also showed good bioavailability rats robust pharmacodynamic effects rabbit model.
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