期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 44, 期 3, 页码 1205-1209出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2008.09.012
关键词
Quinolones; Gatifloxacin; 1,3,4-Thiadiazole; Nitrothiophene; Nitrofuran; Nitroimidazole; Antibacterial activity
资金
- Research Council of Kerman University of Medical Sciences
- Iran National Science Foundation (INSF)
A number of gatifloxacin analogues containing a nitroaryl-1,3,4-thiadiazole moiety attached to the piperazine ring at C-7 position were prepared and evaluated as antibacterial agents against a panel of Gram-positive and Gram-negative bacteria. Among synthesized compounds, nitrofuran analog 6a exhibited more potent inhibitory activity against Gram-positive bacteria including Staphylococcus epidermidis (MIC = 0.0078 mu g/mL), Bacillus subtilis (MIC = 0.0039 mu g/mL), Enterococcus faecalis (MIC = 0.125 mu g/mL) and Micrococcus luteus (MIC = 0.125 mu g/ml.), with respect to other synthesized compounds and reference drug gatifloxacin. The target compounds were also assessed for their cytotoxic activity against normal mouse fibroblast (NIH/3T3) cells using MTT assay. The results indicated that these compounds exhibit antibacterial activity at non-cytotoxic concentrations. (C) 2008 Elsevier Masson SAS. All rights reserved.
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