Cargando…

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...

Descripción completa

Detalles Bibliográficos
Autores principales: Plech, Tomasz, Kaproń, Barbara, Paneth, Agata, Kosikowska, Urszula, Malm, Anna, Strzelczyk, Aleksandra, Stączek, Paweł, Świątek, Łukasz, Rajtar, Barbara, Polz-Dacewicz, Małgorzata
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2015
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
_version_ 1783377241628999680
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
work_keys_str_mv AT plechtomasz determinationoftheprimarymoleculartargetof124triazoleciprofloxacinhybrids
AT kapronbarbara determinationoftheprimarymoleculartargetof124triazoleciprofloxacinhybrids
AT panethagata determinationoftheprimarymoleculartargetof124triazoleciprofloxacinhybrids
AT kosikowskaurszula determinationoftheprimarymoleculartargetof124triazoleciprofloxacinhybrids
AT malmanna determinationoftheprimarymoleculartargetof124triazoleciprofloxacinhybrids
AT strzelczykaleksandra determinationoftheprimarymoleculartargetof124triazoleciprofloxacinhybrids
AT staczekpaweł determinationoftheprimarymoleculartargetof124triazoleciprofloxacinhybrids
AT swiatekłukasz determinationoftheprimarymoleculartargetof124triazoleciprofloxacinhybrids
AT rajtarbarbara determinationoftheprimarymoleculartargetof124triazoleciprofloxacinhybrids
AT polzdacewiczmałgorzata determinationoftheprimarymoleculartargetof124triazoleciprofloxacinhybrids