首页|Synthetic approaches and structural diversity of triazolylbutanols derived from voriconazole in the antifungal drug development

Synthetic approaches and structural diversity of triazolylbutanols derived from voriconazole in the antifungal drug development

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Voriconazole (VCZ) was the first approved triazole antifungal drug with 1-(1H-1,2,4-triazol-1-yl)butan-2-ol substructure. This drug showed a broad spectrum of activity, especially against yeasts and molds, and opened a new avenue toward the novel class of systemic antifungal agents. Modification of 2-fluoropyrimidine in the side chain of VCZ resulted in a newer generation of triazolylbutanols including efinaconazole, albaconazole, ravuconazole, and isavuconazole with the favorable antifungal spectrum, enhanced pharmacokinetic properties, and tolerable toxicity profiles. Due to the importance of triazolylbutanols in the discovery and development of new antifungal agents, in this review we have focused on the synthetic approaches and structural diversity of triazolylbutanols derived from vor-iconazole. This comprehensive review provides highlighting scope for medicinal chemists for the design, synthesis and development of novel potential antifungal drugs having better activity, pharmacokinetic property and toxicity profile.(c) 2022 Elsevier Masson SAS. All rights reserved.

Antifungal activityTriazolesVoriconazoleSynthesisSAR studyIN-VITRO ACTIVITYTRIAZOLE DERIVATIVES SYNTHESISWATER-SOLUBLE PRODRUGSTEREOSELECTIVE-SYNTHESISCRYPTOCOCCUS-NEOFORMANSFLUCONAZOLE RESISTANCEAZOLE ANTIFUNGALSKEY INTERMEDIATELINKED TRIAZOLESORAL TRIAZOLE

Saednia, Shahnaz、Emami, Saeed、Ghobadi, Elham

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Farabi Hosp,Isfahan Univ Med Sci

Fac Pharm,Mazandaran Univ Med Sci

2022

10.1016/j.ejmech.2022.114161

European Journal of Medicinal Chemistry

European Journal of Medicinal Chemistry

CCR
ISSN：0223-5234
年,卷(期)：2022.231
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