Literature DB >> 30897396

Current advances of triazole alcohols derived from fluconazole: Design, in vitro and in silico studies.

Saeed Emami1, Elham Ghobadi2, Shahnaz Saednia3, Seyedeh Mahdieh Hashemi4.   

Abstract

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.
Copyright © 2019 Elsevier Masson SAS. All rights reserved.

Entities:  

Keywords:  Antifungal activity; Azole antifungals; Fluconazole; Lanosterol 14α-demethylase; Triazoles

Mesh:

Substances:

Year:  2019        PMID: 30897396     DOI: 10.1016/j.ejmech.2019.03.020

Source DB:  PubMed          Journal:  Eur J Med Chem        ISSN: 0223-5234            Impact factor:   6.514


  5 in total

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Authors:  Nadipolla Naresh Reddy; Sung-Jen Hung; Merugu Kumara Swamy; Ananthula Sanjeev; Vankadari Srinivasa Rao; Rondla Rohini; Atcha Krishnam Raju; Kuthati Bhaskar; Anren Hu; Puchakayala Muralidhar Reddy
Journal:  Molecules       Date:  2021-03-30       Impact factor: 4.411

  5 in total

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