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

dc.contributor.authorKarpin, George W.en
dc.contributor.authorMorris, David M.en
dc.contributor.authorNgo, Mai T.en
dc.contributor.authorMerola, Joseph S.en
dc.contributor.authorFalkinham, Joseph O. IIIen
dc.contributor.departmentBiological Sciencesen
dc.contributor.departmentChemistryen
dc.contributor.departmentCenter for Drug Discoveryen
dc.date.accessioned2015-11-17T23:19:58Zen
dc.date.available2015-11-17T23:19:58Zen
dc.date.issued2015-06en
dc.description.abstractPentaalkylcyclopentadienyl (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 antibi- otic 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-diamino- cyclohexane 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.en
dc.description.notesContains supplementary information filesen
dc.description.notes2015 Royal Society of Chemistry Open Access Gold Articleen
dc.format.mimetypeapplication/pdfen
dc.identifier.citationMed.Chem.Commun.,2015,6,1471–1478en
dc.identifier.doihttps://doi.org/10.1039/c5md00228aen
dc.identifier.otherDOI: 10.1039/c5md00228aen
dc.identifier.urihttp://hdl.handle.net/10919/64167en
dc.language.isoen_USen
dc.publisherRoyal Society of Chemistryen
dc.rightsCreative Commons Attribution-NonCommercial-NoDerivs 3.0 United Statesen
dc.rights.urihttp://creativecommons.org/licenses/by-nc-nd/3.0/us/en
dc.subjectStaphylococcus aureusen
dc.subjectMRSAen
dc.subjectAntibioticen
dc.subjectAntimicrobialen
dc.subjectTransition metal complexen
dc.titleTransition metal diamine complexes with antimicrobial activity against Staphylococcus aureus and methicillin-resistant S. aureus (MRSA)en
dc.typeArticle - Refereeden
dc.type.dcmitypeTexten

Files

Original bundle
Now showing 1 - 3 of 3
Loading...
Thumbnail Image
Name:
Karpin-2015-Transition metal diamine complexes.pdf
Size:
797.5 KB
Format:
Adobe Portable Document Format
Loading...
Thumbnail Image
Name:
Transition_metal_diamine_supp1.pdf
Size:
113.48 KB
Format:
Adobe Portable Document Format
Description:
Loading...
Thumbnail Image
Name:
Transition_metal_diamine_supp2.pdf
Size:
474.07 KB
Format:
Adobe Portable Document Format
Description:
License bundle
Now showing 1 - 1 of 1
Name:
license.txt
Size:
1.5 KB
Format:
Item-specific license agreed upon to submission
Description: