Current advances of triazole alcohols derived from fluconazole: Design, in vitro and in silico studies.
Antifungal activity
Azole antifungals
Fluconazole
Lanosterol 14α-demethylase
Triazoles
Journal
European journal of medicinal chemistry
ISSN: 1768-3254
Titre abrégé: Eur J Med Chem
Pays: France
ID NLM: 0420510
Informations de publication
Date de publication:
15 May 2019
15 May 2019
Historique:
received:
27
11
2018
revised:
13
01
2019
accepted:
06
03
2019
pubmed:
22
3
2019
medline:
20
4
2019
entrez:
22
3
2019
Statut:
ppublish
Résumé
Currently, the available antifungal agents have significant clinical incompetency in terms of their clinical efficacy, antifungal spectrum, unfavorable pharmacokinetic profiles, substantial side effects and drug-drug interactions. Thus, the optimization and improvement of existing drugs and identification of new antifungal agents are urgently needed. Fluconazole is the first triazole alcohol drug with good in vivo efficacy against yeasts and well-known targets in fungal cells. However, the wide use of fluconazole as a first-line antifungal therapy has led to the development of resistance in clinical isolates of Candida species including Candida albicans and the emerging non-albicans Candida spp. In the last years, extensive efforts inflected to design and discovery of triazole alcohols derived from fluconazole by replacing one triazole ring with the proper side chain. In this paper, we have reviewed the structural modification of fluconazole to pursuit potent triazole alcohols with improved anti-Candida activity, and have highlighted their in vitro activities and in silico studies.
Identifiants
pubmed: 30897396
pii: S0223-5234(19)30231-4
doi: 10.1016/j.ejmech.2019.03.020
pii:
doi:
Substances chimiques
Antifungal Agents
0
Triazoles
0
Fluconazole
8VZV102JFY
Types de publication
Journal Article
Review
Langues
eng
Sous-ensembles de citation
IM
Pagination
173-194Informations de copyright
Copyright © 2019 Elsevier Masson SAS. All rights reserved.