Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 45, Issue 14, Pages 2942-2952Publisher
AMER CHEMICAL SOC
DOI: 10.1021/jm010569q
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A series of diphenyl-substituted heterocycles were synthesized and evaluated by electrophysiological techniques as openers of the cloned mammalian large-conductance, Call-activated potassium (maxi-K) channel. The series was designed from deannulation of known benzimidazolone maxi-K opener NS-004 (2) thereby providing an effective template for obtaining structure-activity-related information. The triazolone ring system was the most studied wherein 4,5-diphenyltriazol-3-one 6d (maxi-K = 158%) was identified as the optimal maxi-K channel opener.
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