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Copper complexes with bioactive ligands Part I--Antimicrobial activity
B Dudová1, D Hudecová, R Pokorný
1Department of Biochemistry and Microbiology, Faculty of Chemical Technology, Slovak University of Technology, 812 37 Bratislava, Slovakia. dudova@chelin.chtf.stuba.sk
Folia Microbiologica
|March 20, 2002
Summary
New copper(II) complexes show significant antimicrobial activity against bacteria and fungi. The most effective complex, Cu(2-MeSNic)2(MeNia)2.4H2O, demonstrated potent antistaphylococcal and antifungal properties without mutagenicity.
Area of Science:
- Coordination Chemistry
- Antimicrobial Agents
- Medicinal Inorganic Chemistry
Background:
- Copper(II) complexes are explored for their diverse biological activities.
- Nicotinamide derivatives offer potential as ligands in coordination chemistry.
- Understanding structure-activity relationships is crucial for developing new therapeutic agents.
Purpose of the Study:
- To synthesize and characterize novel copper(II) complexes with 2-methylthionicotinate and various nicotinamide derivatives.
- To evaluate the antimicrobial and antifungal properties of these new complexes.
- To investigate the effect of these complexes on nucleic acid and protein biosynthesis.
Main Methods:
- Synthesis and characterization of copper(II) complexes.
- Antimicrobial susceptibility testing against Gram-positive (Staphylococcus aureus) and Gram-negative (Escherichia coli) bacteria.
- Antifungal activity testing against Candida parapsilosis.
- Assessment of effects on nucleic acid and protein biosynthesis using radiolabeled precursors (14C-adenine and 14C-leucine).
- Mutagenicity testing.
Main Results:
- Novel copper(II) complexes of 2-methylthionicotinate with N-methyl-nicotinamide, nicotinamide, isonicotinamide, and ethyl nicotinate were synthesized.
- Gram-negative bacteria (E. coli) showed higher resistance than Gram-positive bacteria (S. aureus).
- Cu(2-MeSNic)2(MeNia)2.4H2O exhibited significant antistaphylococcal activity (IC50 1.3 mmol/L).
- Cu(2-MeSNic)2.H2O and Cu(2-MeSNic)2(MeNia)2.4H2O showed potent antifungal activity against Candida parapsilosis (IC50 1.4 and 1.5 mmol/L, respectively).
- Nucleic acid biosynthesis was more sensitive to Cu(2-MeSNic)2(Nia)2.2H2O (IC50(Ade) 0.31 mmol/L) than protein biosynthesis (IC50(Leu) 9.94 mmol/L).
- The active copper(II) complexes displayed no mutagenic activity.
Conclusions:
- The synthesized copper(II) complexes possess significant antimicrobial and antifungal properties.
- The activity varies depending on the bacterial or fungal species and the specific complex structure.
- The complexes interfere with nucleic acid biosynthesis, offering a potential mechanism for their antimicrobial action.
- The absence of mutagenicity suggests a favorable safety profile for further investigation.