title: Determination of the primary molecular target of 1,2,4-triazole-ciprofloxacin hybrids.
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.
authors: Department of Organic Chemistry, Faculty of Pharmacy, Medical University, Chodzki 4A, Lublin 20-093, Poland. tomasz.plech@umlub.pl.
authors: Tomasz
authors: T
authors: Plech
authors: Department of Organic Chemistry, Faculty of Pharmacy, Medical University, Chodzki 4A, Lublin 20-093, Poland. baska_k@o2.pl.
authors: Barbara
authors: B
authors: Kaproń
authors: Department of Organic Chemistry, Faculty of Pharmacy, Medical University, Chodzki 4A, Lublin 20-093, Poland. agata.paneth@umlub.pl.
authors: Agata
authors: A
authors: Paneth
authors: Department of Pharmaceutical Microbiology, Faculty of Pharmacy, Medical University, Chodzki 1, Lublin 20-093, Poland. u.kosikowska@umlub.pl.
authors: Urszula
authors: U
authors: Kosikowska
authors: Department of Pharmaceutical Microbiology, Faculty of Pharmacy, Medical University, Chodzki 1, Lublin 20-093, Poland. anna.malm@umlub.pl.
authors: Anna
authors: A
authors: Malm
authors: Department of Genetics of Microorganisms, University of Lodz, Banacha 12/16, Lodz 90-237, Poland. ola.strzelczyk@wp.pl.
authors: Aleksandra
authors: A
authors: Strzelczyk
authors: Department of Genetics of Microorganisms, University of Lodz, Banacha 12/16, Lodz 90-237, Poland. pstaczek@biol.uni.lodz.pl.
authors: Paweł
authors: P
authors: Stączek
authors: Department of Virology, Faculty of Medicine, Medical University, Chodźki 1, Lublin 20-093, Poland. lukasz.swiatek@umlub.pl.
authors: Łukasz
authors: Ł
authors: Świątek
authors: Department of Virology, Faculty of Medicine, Medical University, Chodźki 1, Lublin 20-093, Poland. b.rajtar@umlub.pl.
authors: Barbara
authors: B
authors: Rajtar
authors: Department of Virology, Faculty of Medicine, Medical University, Chodźki 1, Lublin 20-093, Poland. malgorzata.polz-dacewicz@umlub.pl.
authors: Małgorzata
authors: M
authors: Polz-Dacewicz
mesh_terms: D000900:Anti-Bacterial Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D002939:Ciprofloxacin / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D004250:DNA Topoisomerases, Type II / Q000187:drug effects; D006090:Gram-Negative Bacteria / Q000187:drug effects; D006094:Gram-Positive Bacteria / Q000187:drug effects; D057809:HEK293 Cells; D006801:Humans; D013329:Structure-Activity Relationship; D059005:Topoisomerase II Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D014230:Triazoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D000900:Anti-Bacterial Agents; D059005:Topoisomerase II Inhibitors; D014230:Triazoles; C045575:1,2,4-triazole; D002939:Ciprofloxacin; D004250:DNA Topoisomerases, Type II