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Conazoles.
Jan Heeres1, Lieven Meerpoel, Paul Lewi
1Leemskuilen 18, B-2350 Vosselaar, Belgium. jan@heeres.be
Molecules (Basel, Switzerland)
|July 27, 2010
Summary
This review details the development of conazole antifungals, starting from miconazole. It covers the discovery of orally active azole antifungals like ketoconazole and fluconazole.
Area of Science:
- Medicinal Chemistry
- Pharmacology
- Mycology
Background:
- Miconazole, an early broad-spectrum antifungal, was primarily used topically.
- Its in vitro activity spurred the development of more potent antifungal agents.
- This led to the creation of orally active azole antifungals.
Purpose of the Study:
- To provide a historical overview of analog-based drug discovery for miconazole and related compounds.
- To focus on marketed azole antifungals ending in "conazole".
- To describe the chemistry, activity, pharmacology, and clinical uses of these agents.
Main Methods:
- Literature review of historical drug discovery.
- Analysis of chemical structures and antifungal properties.
- Compilation of pharmacological and clinical data.
Main Results:
- Miconazole's limitations led to the design of potent "conazole" antifungals.
- Marketed conazoles include ketoconazole, itraconazole, posaconazole, fluconazole, and voriconazole.
- These agents exhibit broad-spectrum antifungal activity and varied clinical applications.
Conclusions:
- The evolution from miconazole to modern conazoles represents significant advancements in antifungal therapy.
- Analog-based design has successfully yielded orally available and potent antifungal drugs.
- Marketed conazoles offer diverse options for treating fungal infections.
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