選択毒性に関する研究(第8報) : 1,2,4-チアジアゾール環の生物活性

概要

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Over 60 kinds of 1,2,4-thiadiazole derivatives were synthesized and their biological activities were examined. It was found that 3-methyl-5-(p-chlorophenylsulfonyl)-1,2,4-thiadiazole and 3-methyl-5-(p-tolylsulfonyl)-1,2,4-thiadiazole had the most powerful antimicrobial activity. Among the biological activities of these ring derivatives, the antimicrobial activity of the 5-phenylsulfonyl substituent seemed to depend on the-SO_2-group and its conversion to the -NH-, -O-, or -S- type markedly reduced the effect. Introduction of a substituent in the para position of the benzenesulfonyl group had little effect on the antimicrobial activity but substitution of Cl with CH_3 increased nematocidal effect while conversion to -SCN further increased this activity. In contrast, acaricidal activity was decreased in the -SO_2- form and became effective in -S- form. Antifungal activity was tested by animal experiment. The compounds were effective against Trichophyton but ineffective against Candida. Toxicity and pharmacological tests revealed that these compounds had comparatively low toxicity.
社団法人日本薬学会の論文
1968-11-25