期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 170, 期 -, 页码 173-194出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2019.03.020
关键词
Antifungal activity; Azole antifungals; Fluconazole; Triazoles; Lanosterol 14 alpha-demethylase
资金
- Research Council of Mazandaran University of Medical Sciences, Sari, Iran [5018]
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. (C) 2019 Elsevier Masson SAS. All rights reserved.
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