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Updated: Aug 5, 2026
08:43
Protocol for the Synthesis of Ortho-trifluoromethoxylated Aniline Derivatives
Published on: January 19, 2016
Click Chemistry Approach to Derivatisation of Fluconazole
Michał Janowski1, Oleg M Demchuk2, Sylwia Andrzejczuk3
1Doctoral School, Medical University of Lublin, Chodzki 7, 20-093 Lublin, Poland.
Molecules (Basel, Switzerland)
|July 28, 2026
Summary
New fluconazole derivatives were synthesized to combat antimicrobial resistance. Some compounds demonstrated potent antifungal activity with low toxicity against key Candida species.
Area of Science:
- Medicinal Chemistry
- Organic Synthesis
- Antimicrobial Drug Discovery
Background:
- Antimicrobial resistance is a growing global health threat, necessitating novel therapeutic agents.
- Fluconazole is a widely used antifungal, but resistance is increasing.
- Development of new antifungal agents with improved efficacy and safety profiles is crucial.
Purpose of the Study:
- To design and synthesize novel fluconazole derivatives.
- To evaluate the antifungal activity of these derivatives against clinically relevant Candida species.
- To assess the toxicity profile of the synthesized compounds.
Main Methods:
- Synthesis of fluconazole derivatives via esterification and copper-catalyzed azide-alkyne cycloaddition (CuAAC).
- Optimization of the copper(I) catalyst system using copper(II) palmitate and ascorbic acid.
- Antifungal activity testing against reference strains of Candida spp. (e.g., C. albicans, C. auris).
- Cytotoxicity assessment using MTT-based cell viability assays.
Main Results:
- Successful synthesis of a series of new fluconazole derivatives.
- Identification of compounds exhibiting significant antifungal activity against tested Candida strains.
- Demonstration of low toxicity for some derivatives in cell viability assays.
- Specific activity noted against strains like Candida albicans and Candida auris.
Conclusions:
- The synthesized fluconazole derivatives represent promising candidates for new antifungal therapies.
- The developed synthetic strategy is effective for generating novel antifungal agents.
- Further investigation into these low-toxicity, high-activity compounds is warranted to combat resistant fungal infections.
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