TY - JOUR
TI - Synthesis and preliminary biological evaluation of antibacterial and antifungal 5-arylidene tetramic acid-cadmium(II) complexes
AU - Matiadis, D.
AU - Stefanou, V.
AU - Tsironis, D.
AU - Panagiotopoulou, A.
AU - Igglessi-Markopoulou, O.
AU - Markopoulos, J.
JO - Archiv der Pharmazie
PY - 2021
VL - 354
TODO - 12
SP - null
PB - John Wiley and Sons Inc
SN - 0365-6233, 1521-4184
TODO - 10.1002/ardp.202100305
TODO - 2 pyrrolidone derivative;  antifungal agent;  antiinfective agent;  cadmium;  tetramic acid, bacterium;  chemistry;  drug effect;  fungus;  hemolysis;  human;  microbial sensitivity test;  structure activity relation;  synthesis, Anti-Bacterial Agents;  Antifungal Agents;  Bacteria;  Cadmium;  Fungi;  Hemolysis;  Humans;  Microbial Sensitivity Tests;  Pyrrolidinones;  Structure-Activity Relationship
TODO - The synthesis and biological evaluation of 5-arylidene-N-acetyl-tetramic acids cadmium(II) complexes are reported. Eleven novel compounds were prepared, characterized by nuclear magnetic resonance experiments and screened for their antimicrobial activity against five bacterial species (Escherichia coli, Klebsiella pneumoniae, Acinetobacter baumannii, Pseudomonas aeruginosa, and methicillin-resistant Staphylococcus aureus [MRSA]) and two fungi (Candida albicans and Cryptococcus neoformans). The complexes showed similar or enhanced activities against MRSA in comparison to the corresponding ligands and, additionally, promising antifungal activities against C. neoformans. The most active compounds 3c and 3h showed remarkable activities against MRSA (minimum inhibitory activity [MIC] values of 32 and 4 μg/ml, respectively) and C. neoformans (MIC values of 8 and 16 μg/ml, respectively), accompanied by no human cell toxicity and hemolytic activity within the tested concentration range. The results demonstrate that appropriately functionalized tetramic acids attached with lipophilic alkanoyl chain and after complexation with cadmium(II) ions may act as valuable lead compounds for further investigations toward the development of novel antibacterial and/or antifungal agents. © 2021 Deutsche Pharmazeutische Gesellschaft
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