Abstract

SummarySummaryNovelty: Novel benzimidazoles are disclosed as K+ channel activators. These compounds are said to be useful for the treatment of convulsions, asthma, hypertension and ischaemia.Biology: Activity as potent openers of the high conductance, Ca-activated, K+ channel was demonstrated in vitro using NIE-115 neuroblastoma cells. Test compound-induced hyperpolarization was —14 mV at a dose of 30 μM. Further tests were performed on inside-out patches of cerebellar granule cell membrane, cultured bovine aortic and guinea pig tracheal smooth muscle cells; these tests showed that the K+ channel was significantly activated.Chemistry: Eighteen examples are given for preparation of the compounds by conventional methods. Characterization is by mp. The specified compound is 1-(5-chloro-2-hydroxyphenyl)-5-trifluoromethyl-1,3-dihydro-2H-benzimidazol-2-one.Structure:

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