Novel linezolid-based oxazolidinones as potent anticandidiasis and antitubercular agents.
Anticandidiasis
Antifungal
Antitubercular
Molecular dynamics
Oxazolidinone
Pharmacophore modeling
Journal
Bioorganic chemistry
ISSN: 1090-2120
Titre abrégé: Bioorg Chem
Pays: United States
ID NLM: 1303703
Informations de publication
Date de publication:
09 2022
09 2022
Historique:
received:
20
02
2022
revised:
08
05
2022
accepted:
08
05
2022
pubmed:
23
5
2022
medline:
22
6
2022
entrez:
22
5
2022
Statut:
ppublish
Résumé
The quest for new antifungal and antitubercular drugs is a need of the hour because of morbid co-pathogenesis and an increase in immunocompromised patients. One of the ways forward is to explore and repurpose the established pharmacophores for the desired application. Oxazolidinones are well-known antibacterial agents, with few investigations reported to exploit their antifungal properties. Herein, we report the design and synthesis of a series of linezolid-based oxazolidinones as potent anticandidiasis and antitubercular agents. Studies revealed that two of the novel oxazolidinones 2 and 3a exhibited excellent anticandidiasis activity against different Candida fungus strains, superior to standard drugs. Mechanistic and docking studies revealed that oxazolidinones were better inhibitors of the ergosterol biosynthesis pathway than the controls used. In addition, the oxazolidinones 2 and 3a also exhibited prominent inhibitory activity against M. tuberculosis H
Identifiants
pubmed: 35598571
pii: S0045-2068(22)00274-7
doi: 10.1016/j.bioorg.2022.105869
pii:
doi:
Substances chimiques
Anti-Bacterial Agents
0
Antifungal Agents
0
Antitubercular Agents
0
Oxazolidinones
0
Linezolid
ISQ9I6J12J
Types de publication
Journal Article
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM
Pagination
105869Informations de copyright
Copyright © 2022 Elsevier Inc. All rights reserved.