Studies on gastric antiulcer active agents. III. Synthesis of 1-substituted 4-(5-tetrazolyl)thio-1-butanones and related compounds.
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.
Uchida
M
M
Komatsu
M
M
Morita
S
S
Kanbe
T
T
Yamasaki
K
K
Nakagawa
K
K
D000818:Animals; D000897:Anti-Ulcer Agents / Q000138:chemical synthesis*; D001393:Azoles / Q000138:chemical synthesis*; D055598:Chemical Phenomena; D002621:Chemistry; D051381:Rats; D013276:Stomach Ulcer / Q000188:drug therapy*; D013329:Structure-Activity Relationship; D013777:Tetrazoles / Q000138:chemical synthesis* / Q000494:pharmacology
D000897:Anti-Ulcer Agents; D001393:Azoles; D013777:Tetrazoles; C060883:1-cyclohexyl-4-(1-phenyl-5-tetrazolyl)thio-1-butanone