publication . Article . 2021

In vivo Active Organometallic-containing Antimycotic Agents

Riccardo Rubbiani; Tobias Weil; Noemi Tocci; Luciano Mastrobuoni; Severin Jeger; Marco Moretto; James Ng; Yan Lin; Jeannine Hess; Stefano Ferrari; ...
Open Access English
  • Published: 08 Jul 2021
  • Publisher: HAL CCSD
Abstract
Fungal infections represent a global problem, notably for immunocompromised patients in hospital, COVID-19 patient wards and care home settings, and the ever-increasing emergence of multidrug resistant fungal strains is a sword of Damocles hanging over many healthcare systems. Azoles represent the mainstay of antifungal drugs, and their mode of action involves the binding mode of these molecules to the fungal lanosterol 14α-demethylase target enzyme. In this study, we have prepared and characterized four novel organometallic derivatives of the frontline antifungal drug fluconazole (1a–4a). Very importantly, enzyme inhibition and chemogenomic profiling demonstrat...
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Subjects
free text keywords: Bioorganometallic Chemistry, Antifungals, Medicinal Inorganic Chemistry, [CHIM.THER]Chemical Sciences/Medicinal Chemistry, Chemistry, Settore BIO/10 - BIOCHIMICA
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Funded by
EC| PhotoMedMet
Project
PhotoMedMet
Towards Novel Inert (Photo-)toxic Ru(II) Polypyridyl Complexes
  • Funder: European Commission (EC)
  • Project Code: 681679
  • Funding stream: H2020 | ERC | ERC-COG
,
SNSF| Ruthenium Complexes for the Treatment of Protozoan Diseases of Medical and Veterinary Importance
Project
  • Funder: Swiss National Science Foundation (SNSF)
  • Project Code: CRSII5_173718
  • Funding stream: Programmes | Sinergia
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