Synthesis and biological evaluation of fluconazole analogs with triazole-modified scaffold as potent antifungal agents

Bioorganic & Medicinal Chemistry
Seyedeh Mahdieh HashemiSaeed Emami

Abstract

In order to find new azole antifungals, we have recently designed a series of triazole alcohols in which one of the 1,2,4-triazol-1-yl group in fluconazole structure has been replaced with 4-amino-5-aryl-3-mercapto-1,2,4-triazole motif. In this paper, we focused on the structural refinement of the primary lead, by removing the amino group from the structure to achieve 5-aryl-3-mercapto-1,2,4-triazole derivatives 10a-i and 11a-i. The in vitro antifungal susceptibility testing of title compounds demonstrated that most compounds had potent inhibitory activity against Candida species. Among them, 5-(2,4-dichlorophenyl)triazole analogs 10h and 11h with MIC values of <0.01 to 0.5μg/mL were 4-256 times more potent than fluconazole against Candida species.

Citations

Jan 31, 2016·European Journal of Medicinal Chemistry·Adile AyatiAlireza Foroumadi
Apr 24, 2018·Future Medicinal Chemistry·Kamran MotahariSaeed Emami
Oct 22, 2016·MedChemComm·Huy X NgoKeith D Green
Mar 7, 2020·Chemical Society Reviews·Kaitlind C HowardSylvie Garneau-Tsodikova
Feb 7, 2020·Future Science OA·Mohd Sajjad Ahmad KhanMohammad Zubair Alam
Aug 6, 2021·Journal of Basic Microbiology·Saraswathi NagarajShoba Narayan

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