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Updated: Aug 20, 2025
08:54
Broth Microdilution In Vitro Screening: An Easy and Fast Method to Detect New Antifungal Compounds
Published on: February 14, 2018
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New Antifungal Agents with Azole Moieties
Melissa Martins Teixeira1,2,3, Diogo Teixeira Carvalho1,4, Emília Sousa1,3
1Laboratory of Organic and Pharmaceutical Chemistry, Department of Chemical Sciences, Faculty of Pharmacy, University of Porto, 4050-313 Porto, Portugal.
Pharmaceuticals (Basel, Switzerland)
|November 24, 2022
Summary
Novel antifungal azole drugs are crucial due to rising fungal resistance and immunocompromised patients. This review highlights promising new azole developments in clinical trials, including 1,2,3-triazole conjugates, for effective fungal infection treatment.
Area of Science:
- Mycology
- Medicinal Chemistry
- Pharmacology
Background:
- Fungal infections pose significant global health challenges, increasing hospitalization and mortality.
- Emerging antifungal resistance and a growing immunocompromised population necessitate novel therapeutic agents.
- Azole drugs, while effective, face limitations due to acquired resistance and tolerance in fungal strains.
Purpose of the Study:
- To review promising new azole-based antifungal agents currently in clinical trials.
- To consolidate in vitro, in vivo, and toxicity data for novel antifungal candidates.
- To explore structure-activity relationships (SAR) and emerging antifungal scaffolds.
Main Methods:
- Literature review of scientific databases for azole antifungals in clinical development.
- Analysis of in vitro and in vivo efficacy data against various fungal pathogens.
- Inclusion of complementary assays: toxicity, susceptibility testing, and molecular docking studies.
Main Results:
- Several novel azole structures are in clinical trials or nearing approval, demonstrating broad-spectrum antifungal activity.
- 1,2,3-triazole natural product conjugates show significant promise as new antifungal agents.
- Structure-activity relationship (SAR) studies reveal distinct pharmacophores and design strategies for potent azoles.
Conclusions:
- The azole scaffold remains a privileged structure for antifungal drug discovery.
- Innovative azole derivatives, including triazole conjugates, offer new hope against resistant fungal infections.
- Continued research into novel azoles is vital to expand the antifungal treatment arsenal.
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