期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 24, 期 1, 页码 308-313出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2013.11.013
关键词
Antibacterial; Triazole; Human serum albumin; Naphthalimide; DNA
资金
- National Natural Science Foundation of China [21172181, 21372186, 81350110338, 81250110554]
- key program from Natural Science Foundation of Chongqing [CSTC2012jjB10026]
- Specialized Research Fund for the Doctoral Program of Higher Education of China [SRFDP20110182110007]
- Research Funds for the Central Universities [XDJK2012B026]
- Natural Science Foundation of the Guizhou Province of China [LKB[2012]05]
- Early Career Development Fellowship Program of Bijie University [20102002]
A series of 1,2,3-triazole-derived naphthalimides as a novel type of potential antimicrobial agents were synthesized and characterized by IR, NMR and HRMS spectra. All the new compounds were screened for their antimicrobial activity against four Gram-positive bacteria, four Gram-negative bacteria and three fungi. Bioactive assay manifested that 3,4-dichlorobenzyl compound 9e and its corresponding hydrochloride 11e showed better anti-Escherichia coli activity than Norfloxacin and Chloromycin. Preliminary research revealed that compound 9e could effectively intercalate into calf thymus DNA to form compound 9e-DNA complex which might block DNA replication and thus exert antimicrobial activities. Human serum albumin could effectively store and carry compound 9e by electrostatic interaction. (C) 2013 Published by Elsevier Ltd.
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