新型巯基蛋白酶抑制剂THTT衍生物的抗微生物活性

Antimicrobial activities of a kind of MPI-THTT derivetives

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 -2 H-1,3 ,5 -噻二嗪 -2 -硫酮环的化合物(Tetrahydro-2 H-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 G-菌对 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、伤寒沙门菌的抑菌活性较好 ;而对 G+菌的金黄色葡萄球菌的抑菌活性最强。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 。

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.