4.6 Article

Synthesis, characterization and antimicrobial activity of N-acetyl-3-acetyl-5-benzylidene tetramic acid-metal complexes. X-ray analysis and identification of the Cd(II) complex as a potent antifungal agent

期刊

JOURNAL OF INORGANIC BIOCHEMISTRY
卷 194, 期 -, 页码 65-73

出版社

ELSEVIER SCIENCE INC
DOI: 10.1016/j.jinorgbio.2019.02.008

关键词

Tetramic acid; Pyrrolidine-2,4-dione; Metal complex; Antibacterial activity; Antifungal activity; Crystal structure

资金

  1. Wellcome Trust (UK)
  2. University of Queensland (Australia)
  3. Operational Programme Competitiveness, Entrepreneurship and Innovation (NSRF 2014-2020) [MIS 5002567]
  4. European Union (European Regional Development Fund)
  5. Greek State Scholarship Foundation
  6. SIEMENS
  7. Carlsberg Foundation [CF15-0675]
  8. University of Southern Denmark/Danish Council for Independent Research Natural Sciences [12-124985]

向作者/读者索取更多资源

This study aims at the further expansion of knowledge on the antimicrobial activities of the tetramic acid moiety and the effect of metal complexation. Complexes of the N-acetyl-3-acetyl-5-benzylidenetetramic acid with Mn, Co, Ni, Cu, Zn and Cd were synthesized and screened against 5 key ESKAPE pathogens (Escherichia coli, methicillin-resistant Staphylococcus aureus (MRSA), Klebsiella pneumoniae, Acinetobacter baumannii and Pseudomonas aeruginosa) and 2 fungi (Cryptococcus neoformans and Candida albicans). The cadmium complex was found to effectively inhibit the fungus Cryptococcus neoformans with minimum inhibitory concentration (MIC) of 8 mu g/mL, with no human cell toxicity and hemolytic activity within the tested concentration range. The biologically active tetramic acid-cadmium complex was structurally characterized by single-crystal X-ray analysis. Furthermore, the thermal stability of the ligand and the complexes was investigated along with NMR and EPR studies of the Cd(II) and Co(II) complexes respectively.

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