title: Antimicrobial Activity and Urease Inhibition of Schiff Bases Derived from Isoniazid and Fluorinated Benzaldehydes and of Their Copper(II) Complexes.
abstract: In order to evaluate the influence of substitution on biological properties of Schiff bases and their metal complexes, a series of differently substituted fluorine-containing Schiff bases starting from the drug isoniazid (isonicotinylhydrazide) were prepared and their structures were established by single-crystal X-ray diffraction. Also, four copper(II) complexes of these Schiff bases were synthesized. The prepared compounds were evaluated for their antimicrobial activity and urease inhibition. Two of the Schiff bases exerted activity againstC. albicans. All copper(II) complexes showed excellent inhibitory properties against jack bean urease, considerably better than that of the standard inhibitor acetohydroxamic acid.
authors.affiliation: Department of Chemical Theory of Drugs, Faculty of Pharmacy, Comenius University, Kalinčiakova 8, SK-832 32 Bratislava, Slovakia. habala@fpharm.uniba.sk.
authors.forename: Ladislav
authors.initials: L
authors.lastname: Habala
authors.affiliation: Department of Chemical Theory of Drugs, Faculty of Pharmacy, Comenius University, Kalinčiakova 8, SK-832 32 Bratislava, Slovakia. varenyi@fpharm.uniba.sk.
authors.forename: Samuel
authors.initials: S
authors.lastname: Varényi
authors.affiliation: Department of Cellular and Molecular Biology of Drugs, Faculty of Pharmacy, Comenius University, Kalinčiakova 8, SK-832 32 Bratislava, Slovakia. bilkova@fpharm.uniba.sk.
authors.forename: Andrea
authors.initials: A
authors.lastname: Bilková
authors.affiliation: Department of Chemical Theory of Drugs, Faculty of Pharmacy, Comenius University, Kalinčiakova 8, SK-832 32 Bratislava, Slovakia. herich@fpharm.uniba.sk.|Department of Physical Chemistry, Faculty of Chemical and Food Technology, Slovak University of Technology, Radlinského 9, SK-812 37 Bratislava, Slovakia. herich@fpharm.uniba.sk.
authors.forename: Peter
authors.initials: P
authors.lastname: Herich
authors.affiliation: Department of Chemical Theory of Drugs, Faculty of Pharmacy, Comenius University, Kalinčiakova 8, SK-832 32 Bratislava, Slovakia. valentova@fpharm.uniba.sk.
authors.forename: Jindra
authors.initials: J
authors.lastname: Valentová
authors.affiliation: Department of Physical Chemistry, Faculty of Chemical and Food Technology, Slovak University of Technology, Radlinského 9, SK-812 37 Bratislava, Slovakia. jozef.kozisek@stuba.sk.
authors.forename: Jozef
authors.initials: J
authors.lastname: Kožíšek
authors.affiliation: Department of Chemical Theory of Drugs, Faculty of Pharmacy, Comenius University, Kalinčiakova 8, SK-832 32 Bratislava, Slovakia. devinsky@fpharm.uniba.sk.
authors.forename: Ferdinand
authors.initials: F
authors.lastname: Devínsky
mesh_terms: D000890:Anti-Infective Agents / Q000494:pharmacology; D001547:Benzaldehydes; D056831:Coordination Complexes / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D003300:Copper; D018360:Crystallography, X-Ray; D004926:Escherichia coli; D054879:Halogenation; D020128:Inhibitory Concentration 50; D007538:Isoniazid; D015394:Molecular Structure; D012545:Schiff Bases / Q000737:chemistry* / Q000494:pharmacology; D013329:Structure-Activity Relationship; D014510:Urease / Q000037:antagonists & inhibitors; D014961:X-Ray Diffraction
chemical_list: D000890:Anti-Infective Agents; D001547:Benzaldehydes; D056831:Coordination Complexes; D012545:Schiff Bases; D003300:Copper; D014510:Urease; D007538:Isoniazid
keywords: antimicrobial activity; copper(II) complexes; fluorine; isoniazid; urease inhibitors