一系列 1,4-dihydro-1,3,5-triazine 衍生物被设计并且综合并且他们的抗菌剂和抗真菌的活动被评估。大多数综合混合物显示出几克积极的细菌的紧张的有势力抑制(包括 multidrug 抵抗临床孤立) 并且克否定的细菌的紧张,与在 2.1-181.2 的范围的最小的禁止的集中(MIC )? mol/L。混合物 7a 和 7c 介绍了大多数有势力对克积极的细菌的禁止的活动(例如,葡萄球菌 aureus 4220 ) ,克否定的细菌(例如, Escherichia coli 1924 ) ,并且真菌 Candida albicans 7535,与 2.1 或 4.1 的 MIC ? mol/L。特别,复合 7a 是大多数有势力,与 2.1 的 MIC ? 对四 multidrug 抵抗的、克积极的细菌的紧张的 mol/L。复合 7a, 7c 和 7f 的细胞毒素的活动在 HepG2 房间被估计,并且结果建议忍受 6-benzyloxynaphthalen 一半的 1,4-dihydro-1,3,5-triazine 衍生物是为新奇抗菌剂代理人的发展的有趣的脚手架。
A series of 1,4-dihydro-1,3,5-triazine derivatives were designed and synthesized and their antibacterial and antifungal activities were evaluated. Most of the synthesized compounds showed potent inhibition of several Gram-positive bacterial strains(including multidrug-resistant clinical isolates) and Gramnegative bacterial strains, with minimum inhibitory concentrations(MICs) in the range of 2.1–181.2 mmol/L. Compounds 7a and 7c presented the most potent inhibitory activities against Grampositive bacteria(e.g., Staphylococcus aureus 4220), Gram-negative bacteria(e.g., Escherichia coli 1924),and the fungus Candida albicans 7535, with MICs of 2.1 or 4.1 mmol/L. Especially, compound 7a was the most potent, with an MIC of 2.1 mmol/L against four multidrug-resistant, Gram-positive bacterial strains.The cytotoxic activity of the compound 7a, 7c and 7f was assessed in HepG2 cells, and the results suggest that 1,4-dihydro-1,3,5-triazine derivatives bearing a 6-benzyloxynaphthalen moiety are interesting scaffolds for the development of novel antibacterial agents.