A diverse set of 3,5-disubstitited tetrahydro-2H-1,3,5-thiadiazine-thiones (THTT) and their ester derivatives were synthesized in good to excellent yields. The ester derivatives were screened for their antibacterial and antifungal potential and compared with their acidic counterparts. Structure-activity relationship revealed that the THTTs with N-3 carboxylic functionality have very promising potential against all tested pathogens in general. However, ester analogues showed suppressed or no activities against the same pathogens thus indicate that these compounds can be used as a template study for the development of improved antimicrobial agents/prodrugs.

中文翻译：

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3,5-二取代的Tetrahydro-2

合成了一组3,5-二取代的四氢-2 H -1,3,5-噻二嗪-硫酮（THTT）及其酯衍生物，收率良好。筛选酯衍生物的抗菌和抗真菌潜力，并与酸性衍生物进行比较。构效关系表明，具有N-3羧基官能团的THTTs具有对抗所有测试病原体的巨大潜力。然而，酯类似物显示出对相同病原体的抑制作用或没有活性，因此表明这些化合物可以用作开发改良的抗菌剂/前药的模板研究。