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 compound
N-[3-{3-(Piperidinomethyl)phenoxy}propyl]butamides 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-1H-tetrazol-5- ylthio)butanamide (5f) was found to possess 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.
Ueda,Ishii,Sinozaki,Seiki,Hatanaka
p. 1430 - 1435
(2007/10/02)
More Articles about upstream products of 136622-10-1