设计、合成及部分 1,3,5-三嗪基脲和硫脲衍生物的抗菌活性评价。

Design, synthesis and evaluation of some 1,3,5-triazinyl urea and thiourea derivatives as antimicrobial agents.

机构信息

Department of Chemistry, School of Science, Gujarat University, Ahmedabad 380 009, Gujarat, India.

出版信息

J Enzyme Inhib Med Chem. 2009 Aug;24(4):960-6. doi: 10.1080/14756360802560966.

PMID:19555172

Abstract

In an effort to establish new candidates with improved antimicrobial activities we report here the synthesis and in vitro biological evaluation of various series of compounds (5a-j) and (7a-j) which were evaluated against two Gram positive (S. aureus, B. subtilis), two Gram negative (S. typhosa, E. coli) strains and a yeast-like fungi (C. albicans) using the micro-dilution procedure. Among the synthesized compounds 2-(cyclohexyl amino)-4-(3,4-dimethoxy phenyl ethyl thioureido)-6-(2-chloro phenyl ureido) s-triazine (7e) and 2-(cyclohexyl amino)-4-(3,4-dimethoxy phenyl ethyl thioureido)-6-(4-chloro phenyl ureido) s-triazine (7g) proved to be effective with MIC (0.019 mg ML(-1)) against S. typhosa & E. coli respectively.

摘要

为了寻找具有改进抗菌活性的新候选药物，我们在此报告了一系列化合物（5a-j）和（7a-j）的合成和体外生物学评估结果，这些化合物通过微量稀释法评估了对两种革兰氏阳性（金黄色葡萄球菌、枯草芽孢杆菌）、两种革兰氏阴性（伤寒沙门氏菌、大肠杆菌）菌株和一种酵母样真菌（白色念珠菌）的活性。在所合成的化合物中，2-（环己基氨基）-4-（3,4-二甲氧基苯基乙基硫脲基）-6-（2-氯苯基脲基）均三嗪（7e）和 2-（环己基氨基）-4-（3,4-二甲氧基苯基乙基硫脲基）-6-（4-氯苯基脲基）均三嗪（7g）对伤寒沙门氏菌和大肠杆菌的 MIC（0.019 mg/mL）分别证明有效。