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Platinum Cyclooctadiene Complexes with Activity against Gram-positive Bacteria

Frei, Angelo; Ramu, Soumya; Lowe, Gabrielle J.; Dinh, Hue; Semenec, Lucie; Elliott, Alysha G.; Zuegg, Johannes; Deckers, Anke 1; Jung, Nicole 1,2; Bräse, Stefan 1,2; Cain, Amy K.; Blaskovich, Mark A. T.
1 Institut für Organische Chemie (IOC), Karlsruher Institut für Technologie (KIT)
2 Institut für Biologische und Chemische Systeme (IBCS), Karlsruher Institut für Technologie (KIT)


Antimicrobial resistance is a looming health crisis, and it is becoming increasingly clear that organic chemistry alone is not sufficient to continue to provide the world with novel and effective antibiotics. Recently there has been an increased number of reports describing promising antimicrobial properties of metal-containing compounds. Platinum complexes are well known in the field of inorganic medicinal chemistry for their tremendous success as anticancer agents. Here we report on the promising antibacterial properties of platinum cyclooctadiene (COD) complexes. Amongst the 15 compounds studied, the simplest compounds Pt(COD)X$_{2}$ (X=Cl, I, Pt1 and Pt2) showed excellent activity against a panel of Gram-positive bacteria including vancomycin and methicillin resistant Staphylococcus aureus. Additionally, the lead compounds show no toxicity against mammalian cells or haemolytic properties at the highest tested concentrations, indicating that the observed activity is specific against bacteria. Finally, these compounds showed no toxicity against Galleria mellonella at the highest measured concentrations. However, preliminary efficacy studies in the same animal model found no decrease in bacterial load upon treatment with Pt1 and Pt2. ... mehr

Verlagsausgabe §
DOI: 10.5445/IR/1000136107
Veröffentlicht am 25.11.2021
DOI: 10.1002/cmdc.202100157
Zitationen: 22
Zitationen: 24
Cover der Publikation
Zugehörige Institution(en) am KIT Institut für Biologische und Chemische Systeme (IBCS)
Institut für Organische Chemie (IOC)
Publikationstyp Zeitschriftenaufsatz
Publikationsdatum 05.10.2021
Sprache Englisch
Identifikator ISSN: 1860-7179, 1860-7187
KITopen-ID: 1000136107
HGF-Programm 43.33.11 (POF IV, LK 01) Adaptive and Bioinstructive Materials Systems
Erschienen in ChemMedChem
Verlag John Wiley and Sons
Band 16
Heft 20
Seiten 3165-3171
Nachgewiesen in Scopus
Web of Science
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