Molecules
Department of Organic Chemistry, Faculty of Pharmacy, Medical University of Lublin, Chodzki 4a, 20-089 Lublin, Poland.
Published: June 2024
Fluconazole (2-(2,4-difluorophenyl)-1,3-bis(1-1,2,4-triazol-1-yl)propan-2-ol), which was patented in 1981 and introduced for commercial use in 1988, is a widely utilized antifungal drug whose mechanism of action involves inhibition of the activity of 14-α lanosterol demethylase. Its safety and effectiveness have established it as one of the most frequently employed antifungal agents. Resistance to azole antifungal drugs is becoming more common. It may be related to a mutation of the gene encoding the enzyme. To address this issue, molecules with modifications in three main regions of fluconazole, namely the hydroxyl group, the aromatic ring, and the 1,2,4-triazole rings, have been synthesized in an attempt to create more potent antifungal drugs. These modifications aim at enhancing the effectiveness against microorganisms and improving pharmacokinetic parameters and safety profiles of the synthesized compounds. The present review explores the synthesis of fluconazole derivatives, accompanied by insights into the results of biological studies evaluating the therapeutic effects of these compounds.
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http://dx.doi.org/10.3390/molecules29122855 | DOI Listing |
J Infect Dev Ctries
December 2024
Department of Emergency Medicine, Faculty of Medicine, Universiti Kebangsaan Malaysia, Kuala Lumpur, Malaysia.
Introduction: Since the dawn of the new millennium, Candida species have been increasingly implicated as a cause of both healthcare-associated as well as opportunistic yeast infections, due to the widespread use of indwelling medical devices, total parenteral nutrition, systemic corticosteroids, cytotoxic chemotherapy, and broad-spectrum antibiotics. Candida tropicalis is a pathogenic Candida species associated with considerable morbidity, mortality, and drug resistance issues on a global scale.
Methodology: We report a case of a 43-year-old man who was admitted to our hospital for further management of severe coronavirus disease 2019 (COVID-19) pneumonia.
Sci Rep
January 2025
Department of Pre-clinic and Applied Animal Science, Faculty of Veterinary Science, Mahidol University, Salaya, Thailand.
This study explores the effectiveness of various antifungal drugs in treating sporotrichosis caused by Sporothrix schenckii, especially in non-wild-type (non-WT) strains. The drugs tested include enilconazole (ENIL), isavuconazole (ISA), posaconazole (POS), terbinafine (TER), and itraconazole (ITC). The study involved in vitro and in vivo tests on 10 WT isolates and eight ITC non-WT isolates.
View Article and Find Full Text PDFNat Commun
January 2025
Department of Respiratory Medicine, Nagasaki University Graduate School of Biomedical Sciences, Nagasaki, Japan.
Multidrug resistance in the pathogenic fungus Candida glabrata is a growing global threat. Here, we study mechanisms of multidrug resistance in this pathogen. Exposure of C.
View Article and Find Full Text PDFJ Colloid Interface Sci
April 2025
State Key Laboratory of Pulp and Paper Engineering, South China University of Technology, Guangzhou 510640, China. Electronic address:
Conventional light-driven antimicrobial strategies of zinc oxide (ZnO) are limited by inadequate illumination in dark environments. In this study, carboxylated cellulose nanocrystals (MCNC) mediated flower-like ZnO (C@Z) with self-promoted reactive oxygen species release under dark is fabricated. The adsorption of Zn ions on MCNC prompts the growth of ZnO along the (002) crystal plane, forming a flower-like hybrid with superior dispersibility and oxygen vacancies compared to MCNC-free ZnO, which exposes the (100) plane.
View Article and Find Full Text PDFMolecules
January 2025
Centro de Ciências Naturais e Humanas, Universidade Federal do ABC, Santo André 09280-560, SP, Brazil.
In the present study, the hexane extract from branches of (Winteraceae) displayed potent activity against parasites (100% mortality of the worms at 200 μg/mL). Bioactivity-guided fractionation afforded, in addition to the previously reported bioactive sesquiterpene 3,6-epidioxy-bisabola-1,10-diene, two chemically related drimane sesquiterpenes-polygodial () and 9-deoxymuzigadial (). The anti- effects for compounds and were determined in vitro, with compound demonstrating significant potency (EC value of 10 μM for both male and female worms), while was inactive.
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