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Synthesis and evaluation of the antibacterial activities of aryl substituted dihydrotriazine derivatives
Bioorganic & Medicinal Chemistry Letters ( IF 2.7 ) Pub Date : 2018-03-16 , DOI: 10.1016/j.bmcl.2018.03.037
Tian-Yi Zhang , Zhan-Kui Yu , Xue-Jun Jin , Ming-Yue Li , Liang-Peng Sun , Chang-Ji Zheng , Hu-Ri Piao

Five series of dihydrotriazine derivatives containing chalcone (13a–i), phenoxy acetophenone (14a–b), benzyl benzene (15a–c), naphthoxyl acetophenone (16a–b) and benzyl naphthalene (17a–h) moieties were designed and synthesized. The antibacterial and antifungal activities of these compounds were evaluated against several strains of Gram-positive and Gram-negative bacteria, as well as a single fungus. Compound 17h was found to be the most potent of all of the compounds tested, with an MIC value of 0.5 μg/mL against several Gram-positive (Staphylococcus aureus 4220 and QRSA CCARM 3505) and Gram-negative (Escherichia coli 1924) strains of bacteria. However, this compound was inactive against Pseudomonas aeruginosa 2742 and Salmonella typhimurium 2421, indicating that its antibacterial spectrum is similar to those of the positive controls gatifloxacin and moxifloxacin. The cytotoxic activity of the compound 13i, 16b and 17h was assessed in Human normal liver cells.



中文翻译:

芳基取代的二氢三嗪衍生物的合成和抗菌活性的评价

设计并合成了包含查尔酮(13a–i),苯氧基苯乙酮(14a–b),苄苯(15a–c),萘氧基苯乙酮(16a–b)和苄基萘(17a–h)部分的五个系列的二氢三嗪衍生物。评估了这些化合物对几种革兰氏阳性和革兰氏阴性细菌菌株以及单一真菌的抗菌和抗真菌活性。发现化合物17h是所有测试化合物中最有效的,对几种革兰氏阳性金黄色葡萄球菌4220和QRSA CCARM 3505)和革兰氏阴性菌(大肠杆菌)的MIC值为0.5μg/ mL1924)菌株。但是,该化合物对铜绿假单胞菌2742和鼠伤寒沙门氏菌2421无活性,表明其抗菌谱与阳性对照加替沙星和莫西沙星相似。在人正常肝细胞中评估了化合物13i16b17h的细胞毒活性。

更新日期:2018-03-16
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