Copper complexes with bioactive ligands Part I--Antimicrobial activity.
Biological properties of new copper(II) complexes of 2-methylthionicotinate (2-MeSNic) of composition Cu(2-MeSNic)2(MeNia)(2).4H2O (where MeNia is N-methyl-nicotinamide), Cu(2-MeSNic)2(Nia)(2).2H2O (where Nia is nicotinamide) and Cu(2-MeSNic)2L2 (where L is isonicotinamide (iNia) or ethyl nicotinate (EtNic)) are reported. Gram(-)-bacteria (Escherichia coli) are more resistant against Cu(II) complexes than Gram(+)-bacteria (Staphylococcus aureus)--significant antistaphylococcal activity was found with Cu(2-MeSNic)2(MeNia)(2).4H2O (IC50 1.3 mmol/L). Candida parapsilosis was most inhibited by Cu(2-MeSNic)2.H2O and Cu(2-MeSNic)2(MeNia)(2).4H2O (IC50 1.4 mmol/L and 1.5 mmol/L, respectively). Biosynthesis of nucleic acids influenced by Cu(2-MeSNic)2(Nia)(2).2H2O indicated by incorporation of 14C-adenine (IC50(Ade) 0.31 mmol/L) is more sensitive than biosynthesis of proteins indicated by incorporation of 14C-leucine (IC50(Leu) 9.94 mmol/L). Cu(II) complexes with expressed antimicrobial activity showed no mutagenic activity.
Dudová
B
B
Department of Biochemistry and Microbiology, Faculty of Chemical Technology, Slovak University of Technology, 812 37 Bratislava, Slovakia. dudova@chelin.chtf.stuba.sk
Hudecová
D
D
Pokorný
R
R
Mikulásová
M
M
Palicová
M
M
Segl'a
P
P
Melník
M
M
D000900:Anti-Bacterial Agents; D000890:Anti-Infective Agents / Q000494:pharmacology*; D002175:Candida / Q000187:drug effects; D003300:Copper / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D004755:Enterobacteriaceae / Q000187:drug effects; D008024:Ligands; D008826:Microbial Sensitivity Tests; D009942:Organometallic Compounds / Q000494:pharmacology*; D013211:Staphylococcus aureus / Q000187:drug effects
D000900:Anti-Bacterial Agents; D000890:Anti-Infective Agents; D008024:Ligands; D009942:Organometallic Compounds; D003300:Copper