新型巯基蛋白酶抑制剂THTT衍生物的抗微生物活性

目的：研制针对各种耐药病原微生物的有效新药，合成一类新的含有四氢－2H－1，3，5－噻二嗪－2－硫酸环的化合物（Tetrahydro-2H-1,3,5-thiadiazine-2-thione,THTT)，并研究其抗微生物活性。方法：用5种G^ 菌和1种对10种新合成的化合物进行了生物活性实验。结果：大部分化合物对供试菌株均具有不同程度的抑制作用，对常见肠道菌如大肠杆菌，志贺菌对甲型副伤寒沙门菌，伤寒沙门菌的力活性较好；而对G^ 菌的金黄色葡萄球菌的力活性最强。其中化合物1，7，8，9，11，13抗菌活性较好。与阳性对照药物磺胺嘧啶钠注射液相比，10种化合物的抗菌活性均强于对照物。但是，铜绿假单胞菌对10种化合物均不敏感。结论：大部分化合物对所选常见致病菌有较好的抑菌活性，同时表明有较宽的抗菌谱，该类化合物值得进一步深入研究。

Antimicrobial activities of a kind of MPI-THTT derivetives

OBJECTIVE:To synthesize and investigate antimicrobial activities of a new kind of compounds having Tetrahydro 2H 1,3,5 thiadiazine 2 thione(THTT). METHOD:5 kinds of G+ bacteria and a kind of G bacterium were used to investigate antimicrobial activities of the 10 kinds of compounds which were first time reported in the world. RESULTS:The activity in vitro of these compounds against 6 kinds of bacteria was tested. Comparing with sulfadiazine sodium, antimicrobial activities of the 10 kinds of compounds were improved significantly, especially the benzal substituent THTT. CONCLUSION:These compounds are worth studying further.