4.6 Article

Determination of the Primary Molecular Target of 1,2,4-Triazole-Ciprofloxacin Hybrids

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

  1. Ministry of Science and Higher Education under Iuventus Plus [IP2014 037473]
  2. Medical University of Lublin (Lublin, Poland)

向作者/读者索取更多资源

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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