Efficient Synthesis and Gastric (H^+/K^+)-ATPase-Inhibitory Activity of 2-Aryl-4,5-dihydro-1H-thieno[3,2-e]benzimidazoles

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A series of 2-aryl-4,5-dihydro-1H-thieno[3,2-e]benzimidazoles (1,2) was prepared by condensation of 5-acylamino-4,5,6,7-tetrahydrobenzo[b]thiophen-4-ones (9,10) with ammonium acetate under azeotropic reaction conditions. Various congeners, N-methyl and N-phenyl analogues (3-5), 4,5-dihydro-1H-thieno[2,3-e]benzimidazoles (6), 4,5-dihydro-1H-thieno[2,3-g]benzoxazoles (7), and 4,5-dihydro-1H-thieno[2,3-g]benzothiazoles (8), were also prepared. Several compounds in this series were shown to be K^+-competitive inhibitors of the gastric (H^+/K^+)-ATPase and more potent inhibitors than SK&F-96067,3-butyryl-8-methoxy-4-(2-tolylamino)quinoline, on pentagastrin-stimulated acid secretion in chronic gastric fistula rats after intraduodenal administration.
公益社団法人日本薬学会の論文
1997-12-15