| Literature DB >> 12086481 |
Jeffrey L Romine1, Scott W Martin, Valentin K Gribkoff, Christopher G Boissard, Steven I Dworetzky, Joanne Natale, Yi Li, Qi Gao, Nicholas A Meanwell, John E Starrett.
Abstract
A series of diphenyl-substituted heterocycles were synthesized and evaluated by electrophysiological techniques as openers of the cloned mammalian large-conductance, Ca(2+)-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.Entities:
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Year: 2002 PMID： 12086481 DOI： 10.1021/jm010569q
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446