Next Article in Journal
Hepatoprotective Triterpene Saponins from the Roots of Glycyrrhiza inflata
Previous Article in Journal
Model Organisms in the Fight against Muscular Dystrophy: Lessons from Drosophila and Zebrafish
Article Menu

Export Article

Open AccessArticle
Molecules 2015, 20(4), 6254-6272; doi:10.3390/molecules20046254

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

1
Department of Organic Chemistry, Faculty of Pharmacy, Medical University, Chodzki 4A, Lublin 20-093, Poland
2
Department of Pharmaceutical Microbiology, Faculty of Pharmacy, Medical University, Chodzki 1, Lublin 20-093, Poland
3
Department of Genetics of Microorganisms, University of Lodz, Banacha 12/16, Lodz 90-237, Poland
4
Department of Virology, Faculty of Medicine, Medical University, Chodźki 1, Lublin 20-093, Poland
*
Author to whom correspondence should be addressed.
Academic Editor: Derek J. McPhee
Received: 1 March 2015 / Revised: 29 March 2015 / Accepted: 1 April 2015 / Published: 9 April 2015
(This article belongs to the Section Medicinal Chemistry)
View Full-Text   |   Download PDF [747 KB, uploaded 9 April 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. View Full-Text
Keywords: fluoroquinolones; gyrase DNA; topoisomerase IV; topoisomerase inhibitors; MTT assay fluoroquinolones; gyrase DNA; topoisomerase IV; topoisomerase inhibitors; MTT assay
Figures

Figure 1

This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

Scifeed alert for new publications

Never miss any articles matching your research from any publisher
  • Get alerts for new papers matching your research
  • Find out the new papers from selected authors
  • Updated daily for 49'000+ journals and 6000+ publishers
  • Define your Scifeed now

SciFeed Share & Cite This Article

MDPI and ACS Style

Plech, T.; Kaproń, B.; Paneth, A.; Kosikowska, U.; Malm, A.; Strzelczyk, A.; Stączek, P.; Świątek, Ł.; Rajtar, B.; Polz-Dacewicz, M. Determination of the Primary Molecular Target of 1,2,4-Triazole-Ciprofloxacin Hybrids. Molecules 2015, 20, 6254-6272.

Show more citation formats Show less citations formats

Related Articles

Article Metrics

Article Access Statistics

1

Comments

[Return to top]

Molecules EISSN 1420-3049 Published by MDPI AG, Basel, Switzerland RSS E-Mail Table of Contents Alert
Back to Top