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Issue 8, 2015
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Transition metal diamine complexes with antimicrobial activity against Staphylococcus aureus and methicillin-resistant S. aureus (MRSA)

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Abstract

Pentaalkylcyclopentadienyl (Cp*R) iridium (Ir) and cobalt (Co) 1,2-diamine complexes were synthesized. Susceptibility of Staphylococcus aureus and recent patient methicillin-resistant S. aureus (MRSA) isolates to the transition metal–diamine complexes were measured by broth microdilution and reported as the MIC and MBC. Hemolytic activities of the transition metal-complexes as well as toxicity toward Vero cells were also measured. The transition metal complex of Cp*RIr with cis-1,2-diaminocyclohexane, had strong antibiotic activity against S. aureus and MRSA (MIC = 4 μg mL−1, MBC = 8 μg mL−1) strains and killed 99% of S. aureus cells in 6 hours. Stronger antibiotic activity was associated with the presence of octyl linked to the cyclopentadienyl group and cyclohexane as the diamine backbone. Activity was greatly diminished by tri- or tetramethylation of the nitrogen of the diamine. A cyclopentadienylcobalt complex of cis-1,2-diaminocyclohexane also showed significant anti-microbial activity against both S. aureus and MRSA strains. The absence of hemolytic activity, Vero cell cytotoxicity and the significant anti-microbial activity of several members of the family of compounds reported suggest this is an area worth further development.

Graphical abstract: Transition metal diamine complexes with antimicrobial activity against Staphylococcus aureus and methicillin-resistant S. aureus (MRSA)

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Publication details

The article was received on 27 May 2015, accepted on 18 Jun 2015 and first published on 22 Jun 2015


Article type: Concise Article
DOI: 10.1039/C5MD00228A
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Citation: Med. Chem. Commun., 2015,6, 1471-1478
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    Transition metal diamine complexes with antimicrobial activity against Staphylococcus aureus and methicillin-resistant S. aureus (MRSA)

    G. W. Karpin, D. M. Morris, M. T. Ngo, J. S. Merola and J. O. Falkinham III, Med. Chem. Commun., 2015, 6, 1471
    DOI: 10.1039/C5MD00228A

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