Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 22, Issue 17, Pages 5363-5366Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2012.07.064
Keywords
Clinafloxacin; Quinolone; 1,2,4-Triazole; Antibacterial; Antifungal
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Funding
- National Natural Science Foundation of China [21172181, 81250110089]
- Natural Science Foundation of Chongqing [CSTC2012jjB10026]
- scientific and technological project in Chongqing (CSTC) [2011AB5001]
- Specialized Research Fund for the Doctoral Program of Higher Education of China [SRFDP 20110182110007]
- Research Funds for the Central Universities [XDJK2011D007, XDJK2012B026]
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A series of clinafloxacin triazole hybrids as a new type of antibacterial and antifungal agents were synthesized for the first time and screened for their antimicrobial efficacy against four Gram-positive bacteria, four Gram-negative bacteria and two fungi by two fold serial dilution technique. The bioactive assay indicated that most of the target compounds displayed broad antimicrobial spectrum and good antibacterial and antifungal activities with low MIC values ranging from 0.25 to 2 mu g/mL against all the tested strains which exhibited comparable or even better efficiency in comparison with the reference drugs Chloramphenicol, Clinafloxacin and Fluconazole, respectively. Notably, some synthesized clinafloxacin triazoles showed stronger efficacy against methicillin-resistant Staphylococcus aureus than their parent Clinafloxacin. (C) 2012 Elsevier Ltd. All rights reserved.
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