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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 c...
Autores principales: | , , , , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
MDPI
2015
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6272816/ https://www.ncbi.nlm.nih.gov/pubmed/25859782 http://dx.doi.org/10.3390/molecules20046254 |
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author | Plech, Tomasz Kaproń, Barbara Paneth, Agata Kosikowska, Urszula Malm, Anna Strzelczyk, Aleksandra Stączek, Paweł Świątek, Łukasz Rajtar, Barbara Polz-Dacewicz, Małgorzata |
author_facet | Plech, Tomasz Kaproń, Barbara Paneth, Agata Kosikowska, Urszula Malm, Anna Strzelczyk, Aleksandra Stączek, Paweł Świątek, Łukasz Rajtar, Barbara Polz-Dacewicz, Małgorzata |
author_sort | Plech, Tomasz |
collection | PubMed |
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. |
format | Online Article Text |
id | pubmed-6272816 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2015 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
spelling | pubmed-62728162018-12-03 Determination of the Primary Molecular Target of 1,2,4-Triazole-Ciprofloxacin Hybrids Plech, Tomasz Kaproń, Barbara Paneth, Agata Kosikowska, Urszula Malm, Anna Strzelczyk, Aleksandra Stączek, Paweł Świątek, Łukasz Rajtar, Barbara Polz-Dacewicz, Małgorzata Molecules Article 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. MDPI 2015-04-09 /pmc/articles/PMC6272816/ /pubmed/25859782 http://dx.doi.org/10.3390/molecules20046254 Text en © 2015 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution license (http://creativecommons.org/licenses/by/4.0/). |
spellingShingle | Article Plech, Tomasz Kaproń, Barbara Paneth, Agata Kosikowska, Urszula Malm, Anna Strzelczyk, Aleksandra Stączek, Paweł Świątek, Łukasz Rajtar, Barbara Polz-Dacewicz, Małgorzata Determination of the Primary Molecular Target of 1,2,4-Triazole-Ciprofloxacin Hybrids |
title | Determination of the Primary Molecular Target of 1,2,4-Triazole-Ciprofloxacin Hybrids |
title_full | Determination of the Primary Molecular Target of 1,2,4-Triazole-Ciprofloxacin Hybrids |
title_fullStr | Determination of the Primary Molecular Target of 1,2,4-Triazole-Ciprofloxacin Hybrids |
title_full_unstemmed | Determination of the Primary Molecular Target of 1,2,4-Triazole-Ciprofloxacin Hybrids |
title_short | Determination of the Primary Molecular Target of 1,2,4-Triazole-Ciprofloxacin Hybrids |
title_sort | determination of the primary molecular target of 1,2,4-triazole-ciprofloxacin hybrids |
topic | Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6272816/ https://www.ncbi.nlm.nih.gov/pubmed/25859782 http://dx.doi.org/10.3390/molecules20046254 |
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