期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 28, 期 9, 页码 1657-1662出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2018.03.037
关键词
Antibacterial activitis; Antifungal activities; Cytotoxicity; Dihydrotriazine
资金
- National Natural Science Foundation of China [81260468, 81460524, 81060257]
- Natural Science Foundation of Jilin Province [20160101218JC]
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 mu g/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. (C) 2018 Elsevier Ltd. All rights reserved.
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