期刊
MOLECULES
卷 20, 期 4, 页码 6254-6272出版社
MDPI AG
DOI: 10.3390/molecules20046254
关键词
fluoroquinolones; gyrase DNA; topoisomerase IV; topoisomerase inhibitors; MTT assay
资金
- Ministry of Science and Higher Education under Iuventus Plus [IP2014 037473]
- Medical University of Lublin (Lublin, Poland)
We have synthesized and examined the antibacterial activity, toxicity and affinity towards bacterial type II topoisomerases of a series of 1,2,4-triazole-ciprofloxacin hybrids. A number of these compounds displayed enhanced activity against Gram-positive and Gram-negative bacteria when compared to ciprofloxacin. The toxic concentrations of the obtained derivatives, evaluated on HEK-293 cells using MTT assay, were much higher than concentrations required to produce antibacterial effect. Finally, the results of enzymatic studies showed that the analyzed compounds demonstrated other preferences as regards primary and secondary molecular targets than ciprofloxacin.
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