title: Synthesis and in vitro activity of 1,2,4-triazole-ciprofloxacin hybrids against drug-susceptible and drug-resistant bacteria.
abstract: A series of novel 1,2,4-triazole-ciprofloxacin hybrids was designed, synthesised and evaluated in vitro against drug-susceptible and drug-resistant bacteria. A significant part of the compounds obtained showed antibacterial activity higher than the activity of ciprofloxacin, both towards Gram-positive and Gram-negative species. Despite relatively small number of synthesised derivatives, it was possible to observe important dependences between their structure and activity.
authors.affiliation: Department of Organic Chemistry, Faculty of Pharmacy, Medical University, Chodźki 4a, 20-093 Lublin, Poland. tomasz.plech@umlub.pl
authors.forename: Tomasz
authors.initials: T
authors.lastname: Plech
authors.forename: Monika
authors.initials: M
authors.lastname: Wujec
authors.forename: Urszula
authors.initials: U
authors.lastname: Kosikowska
authors.forename: Anna
authors.initials: A
authors.lastname: Malm
authors.forename: Barbara
authors.initials: B
authors.lastname: Rajtar
authors.forename: Małgorzata
authors.initials: M
authors.lastname: Polz-Dacewicz
mesh_terms: D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D002478:Cells, Cultured; D002939:Ciprofloxacin / Q000737:chemistry / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D024881:Drug Resistance, Bacterial / Q000187:drug effects*; D006090:Gram-Negative Bacteria / Q000187:drug effects*; D006094:Gram-Positive Bacteria / Q000187:drug effects*; D057809:HEK293 Cells; D006801:Humans; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D013329:Structure-Activity Relationship; D014230:Triazoles / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D000900:Anti-Bacterial Agents; D014230:Triazoles; C045575:1,2,4-triazole; D002939:Ciprofloxacin