Object's details: Determination of the Primary Molecular Target of 1,2,4-Triazole-Ciprofloxacin Hybrids

Provider:Repozytorium Uniwersytetu Łódzkiego

Description

Title:
Determination of the Primary Molecular Target of 1,2,4-Triazole-Ciprofloxacin Hybrids
Creator:
Plech, Tomasz;
Kaproń, Barbara;
Paneth, Agata;
Kosikowska, Urszula;
Malm, Anna;
Strzelczyk, Aleksandra;
Stączek, Paweł;
Świątek, Łukasz;
Rajtar, Barbara;
Polz-Dacewicz, Małgorzata
Contributor:
Plech Tomasz, Department of Organic Chemistry, Faculty of Pharmacy, Medical University Lublin;
Kaproń Barbara, Department of Organic Chemistry, Faculty of Pharmacy, Medical University Lublin;
Paneth Agata, Department of Organic Chemistry, Faculty of Pharmacy, Medical University Lublin;
Kosikowska Urszula, Department of Pharmaceutical Microbiology, Faculty of Pharmacy, Medical University Lublin;
Malm Anna, Department of Pharmaceutical Microbiology, Faculty of Pharmacy, Medical University Lublin;
Strzelczyk Aleksandra, Department of Genetics of Microorganisms, University of Lodz;
Stączek Paweł, Department of Genetics of Microorganisms, University of Lodz;
Świątek Łukasz, Department of Virology, Faculty of Medicine, Medical University Lublin;
Rajtar Barbara, Department of Virology, Faculty of Medicine, Medical University Lublin;
Polz-Dacewicz Małgorzata, Department of Virology, Faculty of Medicine, Medical University Lublin;
ola.strzelczyk@wp.pl;
pstaczek@biol.uni.lodz.pl
Description:
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.;
This research was supported by the Ministry of Science and Higher Education under Iuventus Plus grant No. IP2014 037473. Tomasz Plech is a recipient of the Fellowship for Young Researchers with Outstanding Scientific Achievements from the Medical University of Lublin (Lublin, Poland).
Object availability:
free access
Rights:
Uznanie autorstwa 3.0 Polska;
http://creativecommons.org/licenses/by/3.0/pl
Date:
2015.08.31;
2015.04.09
Type:
Article
Language:
English
Format:
application/pdf
Publisher:
Molecular Diversity Preservation International,
Relation:
Molecules;2015;
20
Subject:
fluoroquinolones;
gyrase DNA;
topoisomerase IV;
topoisomerase inhibitors;
MTT assay
Identifier:
1420-3049;
http://hdl.handle.net/11089/11603 ;doi:10.3390/molecules20046254
Data provider:
Repozytorium Uniwersytetu Łódzkiego

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Object's details: Determination of the Primary Molecular Target of 1,2,4-Triazole-Ciprofloxacin Hybrids

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