Antifungal and Antiparasitic Activities of Metallocene-Containing Fluconazole DerivativesClick to copy article linkArticle link copied!
- Yan LinYan LinChimie ParisTech, PSL University, CNRS, Institute of Chemistry for Life and Health Sciences, Laboratory for Inorganic Chemical Biology, 75005 Paris, FranceMore by Yan Lin
- Gonzalo ScaleseGonzalo ScaleseÁrea Química Inorgánica, Facultad de Química, Universidad de la República, 11800 Montevideo, UruguayMore by Gonzalo Scalese
- Christina A. BulmanChristina A. BulmanDepartment of Pharmaceutical Chemistry, University of California, San Francisco, San Francisco, California 94158, United StatesMore by Christina A. Bulman
- Robin VinckRobin VinckChimie ParisTech, PSL University, CNRS, Institute of Chemistry for Life and Health Sciences, Laboratory for Inorganic Chemical Biology, 75005 Paris, FranceMore by Robin Vinck
- Olivier BlacqueOlivier BlacqueDepartment of Chemistry, University of Zurich, Winterthurerstrasse 190, 8057 Zurich, SwitzerlandMore by Olivier Blacque
- Margot PaulinoMargot PaulinoÁrea Bioinformática, Departamento DETEMA, Facultad de Química, Universidad de la República, 11600 Montevideo, UruguayMore by Margot Paulino
- Andres Ballesteros-CasallasAndres Ballesteros-CasallasÁrea Bioinformática, Departamento DETEMA, Facultad de Química, Universidad de la República, 11600 Montevideo, UruguayMore by Andres Ballesteros-Casallas
- Leticia Pérez DíazLeticia Pérez DíazSección Genómica Funcional, Facultad de Ciencias, Universidad de la República, 11400 Montevideo, UruguayMore by Leticia Pérez Díaz
- Gustavo SalinasGustavo SalinasWorm Biology Lab, Institut Pasteur de Montevideo, 11400 Montevideo, UruguayDepartamento de Biociencias, Facultad de Química, Universidad de la República, 11800 Montevideo, UruguayMore by Gustavo Salinas
- Makedonka Mitreva*Makedonka Mitreva*Email: [email protected]Department of Medicine, Washington University School of Medicine, St. Louis, Missouri 63108, United StatesMore by Makedonka Mitreva
- Tobias Weil*Tobias Weil*Email: [email protected]Research and Innovation Centre, Fondazione Edmund Mach, Via E. Mach 1, 38010 San Michele all’Adige, ItalyMore by Tobias Weil
- Kevin Cariou*Kevin Cariou*Email: [email protected]Chimie ParisTech, PSL University, CNRS, Institute of Chemistry for Life and Health Sciences, Laboratory for Inorganic Chemical Biology, 75005 Paris, FranceMore by Kevin Cariou
- Judy A. Sakanari*Judy A. Sakanari*Email: [email protected]Department of Pharmaceutical Chemistry, University of California, San Francisco, San Francisco, California 94158, United StatesMore by Judy A. Sakanari
- Dinorah Gambino*Dinorah Gambino*Email: [email protected]Área Química Inorgánica, Facultad de Química, Universidad de la República, 11800 Montevideo, UruguayMore by Dinorah Gambino
- Gilles Gasser*Gilles Gasser*Email: [email protected]Chimie ParisTech, PSL University, CNRS, Institute of Chemistry for Life and Health Sciences, Laboratory for Inorganic Chemical Biology, 75005 Paris, FranceMore by Gilles Gasser
Abstract

The search for new anti-infectives based on metal complexes is gaining momentum. Among the different options taken by researchers, the one involving the use of organometallic complexes is probably the most successful one with a compound, namely, ferroquine, already in clinical trials against malaria. In this study, we describe the preparation and in-depth characterization of 10 new (organometallic) derivatives of the approved antifungal drug fluconazole. Our rationale is that the sterol 14α-demethylase is an enzyme part of the ergosterol biosynthesis route in Trypanosoma and is similar to the one in pathogenic fungi. To demonstrate our postulate, docking experiments to assess the binding of our compounds with the enzyme were also performed. Our compounds were then tested on a range of fungal strains and parasitic organisms, including the protozoan parasite Trypanosoma cruzi (T. cruzi) responsible for Chagas disease, an endemic disease in Latin America that ranks among some of the most prevalent parasitic diseases worldwide. Of high interest, the two most potent compounds of the study on T. cruzi that contain a ferrocene or cobaltocenium were found to be harmless for an invertebrate animal model, namely, Caenorhabditis elegans (C. elegans), without affecting motility, viability, or development.
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This article is cited by 2 publications.
- Sara Abdolmaleki, Alireza Aliabadi, Samad Khaksar. Bridging the gap between theory and treatment: Transition metal complexes as successful candidates in medicine. Coordination Chemistry Reviews 2025, 531 , 216477. https://doi.org/10.1016/j.ccr.2025.216477
- Tiansheng Wang, Didier Astruc. Electron-reservoir applications of ferrocenes and other late transition-metal sandwich complexes: Flow batteries, sensing, catalysis, and biomedicine. Coordination Chemistry Reviews 2025, 524 , 216300. https://doi.org/10.1016/j.ccr.2024.216300
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