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Title: Antiulcer agents. II. Synthesis and gastric acid antisecretory activity of N-[3-(3-(piperidinomethyl)phenoxy)propyl]-4-(1-methyl-1H- tetrazol-5-ylthio)butanamide and related compounds. Author: Ueda I, Ishii K, Sinozaki K, Seiki M, Hatanaka M. Journal: Chem Pharm Bull (Tokyo); 1991 Jun; 39(6):1430-5. PubMed ID: 1934163. Abstract: N-[3-(3-(Piperidinomethyl)phenoxy)propyl]butanamides having a 1-methyl-1H-tetrazol-5-ylthio moiety as a pharmacophore and related compounds were prepared and tested for their antisecretory activity against histamine-induced gastric acid secretion in conscious rats with gastric fistulas. Most of the compounds showed antisecretory activity. Among them, N-[3-(3-(piperidinomethyl)phenoxy)propyl]-4-(1-methyl-1 H-tetrazol-5-ylthio)butanamide (5f) was found to posses the most potent activity, and a possibility of isosteric replacement of the methoxycarbonyl group with 1-methyl-1H-tetrazol-5-yl group was indicated. The structure-activity relationships are also discussed.[Abstract] [Full Text] [Related] [New Search]