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

Molecules

Tomasz Plech²  Barbara Kaproń²  Agata Paneth²  Urszula Kosikowska³  Anna Malm³  Aleksandra Strzelczyk¹  Paweł Stၜzek¹  Łukasz Świątek⁴  Barbara Rajtar⁴  Małgorzata Polz-Dacewicz⁴ 

[1] Department of Genetics of Microorganisms, University of Lodz, Banacha 12/16, Lodz 90-237, Poland; E-Mails:;Department of Organic Chemistry, Faculty of Pharmacy, Medical University, Chodzki 4A, Lublin 20-093, Poland; E-Mails:;Department of Pharmaceutical Microbiology, Faculty of Pharmacy, Medical University, Chodzki 1, Lublin 20-093, Poland; E-Mails:;Department of Virology, Faculty of Medicine, Medical University, Chodźki 1, Lublin 20-093, Poland; E-Mails:

关键词: fluoroquinolones;    gyrase DNA;    topoisomerase IV;    topoisomerase inhibitors;    MTT assay;   

DOI  :  10.3390/molecules20046254

来源: mdpi

【 摘 要 】

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.

【 授权许可】

CC BY   
© 2015 by the authors; licensee MDPI, Basel, Switzerland.