Studies on Gastric Antiulcer Active Agents. III. : Synthesis of 1-Substituted 4-(5-Tetrazolyl)thio-1-butanones and Related Compounds

Minoru UCHIDA; Makoto KOMATSU; Seiji MORITA; Toshimi KANBE; Katsuya YAMASAKI; Kazuyuki NAKAGAWA

doi:10.1248/cpb.37.958

Minoru UCHIDA, Makoto KOMATSU, Seiji MORITA, Toshimi KANBE, Katsuya YAMASAKI, Kazuyuki NAKAGAWA

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Keywords: 1-substituted 4-(5-tetrazolyl)thio-1-butanone, antiulcer activity, structure-activity relationship, 1-cyclohexyl-4-(1-phenyl-5-tetrazolyl)thio-1-butanone

JOURNAL FREE ACCESS

1989 Volume 37 Issue 4 Pages 958-961

DOI https://doi.org/10.1248/cpb.37.958

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Abstract

Many 1-substituted 4-(5-tetrazolyl)thio-1-butanones were synthesized and tested for antiulcer activity against acetic acid-induced gastric ulcer in rats. These compounds were prepared by the reaction of 5-mercaptotetrazoles and 4-halogeno-1-butanones. Among them, 1-cyclohexyl-4-(1-phenyl-5-tetrazolyl)thio-1-butanone (VIIIp) was found to have the most potent activity. The structure-activity relationships are discussed.

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