期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 23, 期 11, 页码 3267-3272出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2013.03.118
关键词
Quinolone; Triazole; Antibacterial; Antifungal; DNA
资金
- National Natural Science Foundation of China [21172181]
- Research Fund for International Young Scientists from International (Regional) Cooperation and Exchange Program [81250110089, 81250110554]
- Key Program of Natural Science Foundation of Chongqing [CSTC2012jjB10026]
- Specialized Research Fund for the Doctoral Program of Higher Education of China (SRFDP) [20110182110007]
- Research Funds for the Central Universities [XDJK2011D007, XDJK2012B026]
A novel series of quinolone triazoles were synthesized and characterized by IR, NMR, MS and HRMS spectra. All the newly prepared compounds were screened for their antimicrobial activities against seven bacteria and four fungi. Bioactive assay manifested that most of new compounds exhibited good or even stronger antibacterial and antifungal activities against the tested strains including multi-drug resistant MRSA in comparison with reference drugs Norfloxacin, Chloromycin and Fluconazole. The preliminary interactive investigations of compound 6b with calf thymus DNA by fluorescence and UV-vis spectroscopic methods revealed that compound 6b could effectively intercalate DNA to form compound 6b-DNA complex which might block DNA replication and thus exert its antimicrobial activities. (C) 2013 Elsevier Ltd. All rights reserved.
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