Synthesis and biological evaluation of dihydrotriazine derivatives as potential antibacterial agents
| Autor: | Liang-Peng Sun, Hu-Ri Piao, Yu-Shun Tian, Chang-Ji Zheng, Chao Li, Jia-Jun Li, Tian-Yi Zhang |
|---|---|
| Rok vydání: | 2017 |
| Předmět: |
biology
010405 organic chemistry Chemistry General Chemistry Fungus 010402 general chemistry biology.organism_classification medicine.disease_cause 01 natural sciences 0104 chemical sciences Minimum inhibitory concentration Biochemistry Staphylococcus aureus medicine Moiety Candida albicans Cytotoxicity Escherichia coli Bacteria |
| Zdroj: | Chinese Chemical Letters. 28:1737-1742 |
| ISSN: | 1001-8417 |
| DOI: | 10.1016/j.cclet.2017.05.022 |
| Popis: | 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 Gram-negative 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 Gram-positive 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. |
| Databáze: | OpenAIRE |
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