Citation: Zhang Tian-Yi, Li Chao, Tian Yu-Shun, Li Jia-Jun, Sun Liang-Peng, Zheng Chang-Ji, Piao Hu-Ri. Synthesis and biological evaluation of dihydrotriazine derivatives as potential antibacterial agents[J]. Chinese Chemical Letters, ;2017, 28(8): 1737-1742. doi: 10.1016/j.cclet.2017.05.022 shu

Synthesis and biological evaluation of dihydrotriazine derivatives as potential antibacterial agents

Zhang Tian-Yi ^a,b,1 ,
Li Chao ^a,1 ,
Tian Yu-Shun ^a ,
Li Jia-Jun ^a ,
Sun Liang-Peng ^a ,
Zheng Chang-Ji ^a,, ,
Piao Hu-Ri ^a,,

a.
Key Laboratory of Natural Resources of Changbai Mountain & Functional Molecules, Ministry of Education, Yanbian University College of Pharmacy, Yanji 133000, China
b.
Department of Pharmacy, Jilin Medical University, Jilin 132013, China

Corresponding author: Zheng Chang-Ji, zhengcj@ybu.edu.cn Piao Hu-Ri, piaohr@ybu.edu.cn

Received Date: 8 March 2017
Revised Date: 27 April 2017
Accepted Date: 2 May 2017
Available Online: 29 August 2017

Figures(4)

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 μmol/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 μmol/L. Especially, compound 7a was the most potent, with an MIC of 2.1 μmol/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.
- Antibacterial activitis,
- Antifungal activities,
- Cytotoxicity,
- Minimal inhibitory concentration,
- 1, 4-Dihydro-1, 3, 5-triazine
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