期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 26, 期 24, 页码 5920-5925出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2016.11.001
关键词
Chalcone; Acylhydrazone; Aminoguanidine; Antibacterial activity; Antifungal activity; Anti-inflammatory activity; Cytotoxicity
资金
- National Natural Science Foundation of China [81260468, 81460524, 81060257]
Three novel series of chalcone derivatives containing an aminoguanidine or acylhydrazone moiety were designed, synthesized and evaluated in terms of their antibacterial, antifungal and anti-inflammatory activities. Most of the synthesized compounds showed potent inhibitory activity towards various bacteria and one fungus with minimum inhibitory concentrations (MICs) ranging from 1 to 8 mu g/mL. Compared with our previously reported chalcone derivatives (MICs >64 mu g/mL), these compounds exhibited improved antibacterial activities (MICs = 2 mu g/mL) against Gram-negative bacterial strains (Escherichia coli 1924 and 1356). Compounds 4f and 4h were found to be the most potent with an MIC value of 1 mu g/mL against the Gram-negative bacterial strains Salmonella typhimurium 1926 and the fungus Candida albicans 7535. In addition, compound 4f displayed the most potent anti-inflammatory activity of all of the compounds prepared in the current study with 92.45% inhibition after intraperitoneal administration, making it more potent than the reference drugs indomethacin and ibuprofen. The cytotoxic activity of the compound 4f was assessed in HeLa, Hep3B and L02 cells. (C) 2016 Elsevier Ltd. All rights reserved.
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