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Biguanide iridium(III) complexes with potent antimicrobial activity

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Chen, Feng, Moat, John, McFeely, Daniel, Clarkson, Guy J., Hands-Portman, Ian J., Furner-Pardoe, Jessica P., Harrison, Freya, Dowson, Christopher G. and Sadler, P. J. (2018) Biguanide iridium(III) complexes with potent antimicrobial activity. Journal of Medicinal Chemistry, 61 (16). pp. 7330-7344. doi:10.1021/acs.jmedchem.8b00906

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Official URL: https://doi.org/10.1021/acs.jmedchem.8b00906

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Abstract

We have synthesized novel organoiridium(III) antimicrobial complexes containing a chelated biguanide, including the antidiabetic drug metformin. These 16- and 18-electron complexes were characterized by NMR, ESI-MS, elemental analysis, and X-ray crystallography. Several of these complexes exhibit potent activity against Gram-negative bacteria and Gram-positive bacteria (including methicillin-resistant Staphylococcus aureus (MRSA)) and high antifungal potency toward C. albicans and C. neoformans, with minimum inhibitory concentrations (MICs) in the nanomolar range. Importantly, the complexes exhibit low cytotoxicity toward mammalian cells, indicating high selectivity. They are highly stable in broth medium, with a low tendency to generate resistance mutations. On coadministration, they can restore the activity of vancomycin against vancomycin-resistant Enterococci (VRE). Also the complexes can disrupt and eradicate bacteria in mature biofilms. Investigations of reactions with biomolecules suggest that these organometallic complexes deliver active biguanides into microorganisms, whereas the biguanides themselves are inactive when administered alone.

Item Type: Journal Article
Subjects: R Medicine > RC Internal medicine
Divisions: Faculty of Science > Chemistry
Faculty of Science > Life Sciences (2010- )
SWORD Depositor: Library Publications Router
Library of Congress Subject Headings (LCSH): Hypoglycemic agents, Organoiridium compounds
Journal or Publication Title: Journal of Medicinal Chemistry
Publisher: American Chemical Society (ACS)
ISSN: 1520-4804
Official Date: 23 August 2018
Dates:
DateEvent
23 August 2018Published
2 August 2018Available
2 August 2018Accepted
Volume: 61
Number: 16
Page Range: pp. 7330-7344
DOI: 10.1021/acs.jmedchem.8b00906
Status: Peer Reviewed
Publication Status: Published
Publisher Statement: “This document is the Accepted Manuscript version of a Published Work that appeared in final form in Journal of Medicinal Chemistry, copyright © American Chemical Society after peer review and technical editing by the publisher. To access the final edited and published work see http://pubs.acs.org/page/policy/articlesonrequest/index.html].”
Access rights to Published version: Restricted or Subscription Access
RIOXX Funder/Project Grant:
Project/Grant IDRIOXX Funder NameFunder ID
UNSPECIFIEDWellcome Trusthttp://dx.doi.org/10.13039/100010269
UNSPECIFIEDUniversity of Queenslandhttp://dx.doi.org/10.13039/501100001794
EP/F034210/1 [EPSRC] Engineering and Physical Sciences Research Councilhttp://dx.doi.org/10.13039/501100000266
EP/P030572/1 [EPSRC] Engineering and Physical Sciences Research Councilhttp://dx.doi.org/10.13039/501100000266
EP/M027503/1[EPSRC] Engineering and Physical Sciences Research Councilhttp://dx.doi.org/10.13039/501100000266
UNSPECIFIEDChina Scholarship Councilhttp://dx.doi.org/10.13039/501100004543
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