Synthesis and biological evaluation of dihydrotriazine derivatives as potential antibacterial agents

来源 :Chinese Chemical Letters | 被引量 : 0次 | 上传用户:arsonloupeen
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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. A series of 1,4-dihydro-1,3,5-triazine derivatives were designed and synthesized and their antibacterial and antifungal activities were all 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 the 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 (eg Staphylococcus aureus 4220), Gram-negative bacteria (eg, 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. The cytotoxic activity of the compounds 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-benzyloxynaphthalenyl are interesting scaffolds for the development of novel antibacterial agents.
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