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

Tomasz Plech; Barbara Kaproń; Agata Paneth; Urszula Kosikowska; Anna Malm; Aleksandra Strzelczyk; Paweł Stączek; Łukasz Świątek; Barbara Rajtar; Małgorzata Polz-Dacewicz

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

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.

显示更多 [+]