血吸虫病化学治疗的研究 ⅩⅩⅩⅥ.4-苯基(或烯丙基)-5-(吡嗪-2)-1,2,4-三唑-3-硫酮衍生物的合成

本文报导28个4-苯基(或烯丙基)-5-(吡嗪-2)-1,2,4-三唑-3-硫酮衍生物的合成。这类化合物的合成是以吡嗪甲酸乙酯与水合肼反应得2-吡嗪甲酰肼,再与不同的异硫氰酸酯作用后,在2N氢氧化钠溶液中环合而得Ⅱ或Ⅲ,然后经烷化、酰化及Mannich反应,分别制得相应的化合物。其中Ⅲ₁和Ⅲ₂对感染日本血吸虫小白鼠有明显肝移作用。

Chemotherapeutic studies on schistosomiasis. XXXVI. Synthesis of derivatives of 4-phenyl-and 4-allyl-5-(pyrazinyl-2)-1, 2, 4-triazole-3-thio-ketone

Twenty-eight new derivatives of 4-phenyl-and 4-allyl-5-(pyrazinyl2)-l,2,4-triazole-3-thio-ketone (II and III) were synthesized. The key intermediates 4-phenyl- and 4-allyl-substituted l-(pyrazinyl-2) formyl-thiosemicarbazide were obtained from ethyl-(pyrazinyl-2)-carboxylate by hydrazinolysis and reaction subsequently with phenyl or allyl isothiocyanate. They were cyclized in the presence of 2N sodium hydroxide to form II and III, followed by alkylation, acylation and Mannicb reaction under various suitable conditions to afford the corresponding compounds. After preliminary screening two compounds (III₁, III₂) were found to have pro nounced effect on liver shift of Schistosoma japonica in experimental mice.