胃抗溃疡活性剂的研究。III. 1-取代-4-(5-四唑基)硫代-1-丁酮及相关化合物的合成。
Studies on gastric antiulcer active agents. III. Synthesis of 1-substituted 4-(5-tetrazolyl)thio-1-butanones and related compounds.
作者信息
Uchida M, Komatsu M, Morita S, Kanbe T, Yamasaki K, Nakagawa K
出版信息
Chem Pharm Bull (Tokyo). 1989 Apr;37(4):958-61. doi: 10.1248/cpb.37.958.
PMID:2766419
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.
摘要
合成了许多1-取代的4-(5-四唑基)硫代-1-丁酮，并对其在大鼠中针对乙酸诱导的胃溃疡的抗溃疡活性进行了测试。这些化合物通过5-巯基四唑与4-卤代-1-丁酮反应制备。其中，1-环己基-4-(1-苯基-5-四唑基)硫代-1-丁酮(VIIIp)被发现具有最强的活性。讨论了构效关系。
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