Relationship between the Structures and Cytotoxic Activities of 1,3,4-Thiadiazolo[3,2-a]pyrimidines |
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| Authors: | Masahito Suiko Sakumi Hayashida Seiichiro Nakatsu |
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| Institution: | Department of Agricultural Chemistry, Miyazaki University, Miyazaki 880, Japan |
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| Abstract: | 1,3,4-Thiadiazole derivatives having a partial structure of 2-ethylsulfonyl-7-methyl-5H-1,3,4-thiadiazolo3,2-a]pyrimidin-5-one (TPSO2-2) were synthesized, and their chemical reactivities and biological activities were investigated. TPSO2-2 readily reacted with SH compounds and showed a high inhibitory effect against “SH enzyme,” but 2-acetylamino-5-ethylsulfonyl-1,3,4-thiadiazole (AEST), a TPSO2-2 analog without a pyrimidine structure, did not react with those compounds and showed a smaller inhibitory effect against the enzyme. Furthermore, TPSO2-2 showed a strong anti-yeast activity, while AEST did not. It is presumed that not only the electron-withdrawing sulfonyl group at the 2-position but also the pseudopurine skeleton appear to be responsible for revealing the biological and chemical activities of TPSO2-2. |
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