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

Authors :
Tomasz Plech
Barbara Kaproń
Agata Paneth
Urszula Kosikowska
Anna Malm
Aleksandra Strzelczyk
Paweł Stączek
Łukasz Świątek
Barbara Rajtar
Małgorzata Polz-Dacewicz
Source :
Molecules, Vol 20, Iss 4, Pp 6254-6272 (2015)
Publication Year :
2015
Publisher :
MDPI AG, 2015.

Abstract

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.

Details

Language :
English
ISSN :
14203049
Volume :
20
Issue :
4
Database :
Directory of Open Access Journals
Journal :
Molecules
Publication Type :
Academic Journal
Accession number :
edsdoj.9ed9d1ddb19f403aa0ce750450bd7fda
Document Type :
article
Full Text :
https://doi.org/10.3390/molecules20046254