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Data for Biguanide iridium(III) complexes with potent antimicrobial activity

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Chen, Feng, Moat, John, McFeely, Daniel, Clarkson, Guy J., Hands-Portman, Ian, Furner-Pardoe, Jessica P., Harrison, Freya, Dowson, Christopher G. and Sadler, P. J. (2018) Data for Biguanide iridium(III) complexes with potent antimicrobial activity. [Dataset]

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Official URL: http://wrap.warwick.ac.uk/108273

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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: Dataset
Subjects: R Medicine > RC Internal medicine
Divisions: Faculty of Science, Engineering and Medicine > Science > Chemistry
Faculty of Science, Engineering and Medicine > Science > Life Sciences (2010- )
Type of Data: Zip
Library of Congress Subject Headings (LCSH): Hypoglycemic agents, Organoiridium compounds
Publisher: University of Warwick, Department of Chemistry
Official Date: 23 August 2018
Dates:
DateEvent
23 August 2018Published
2 August 2018Available
2 August 2018Accepted
Status: Not Peer Reviewed
Publication Status: Published
Media of Output (format): Files
Access rights to Published version: Open Access (Creative Commons)
Description:

Complexes 1-14

Date of first compliant deposit: 17 September 2018
Date of first compliant Open Access: 2 August 2019
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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