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Conazoles

Overview
Journal Molecules
Publisher MDPI
Specialty Biology
Date 2010 Jul 27
PMID 20657432
Citations 32
Authors
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Abstract

This review provides a historical overview of the analog based drug discovery of miconazole and its congeners, and is focused on marketed azole antifungals bearing the generic suffix "conazole". The antifungal activity of miconazole, one of the first broad-spectrum antimycotic agents has been mainly restricted to topical applications. The attractive in vitro antifungal spectrum was a starting point to design more potent and especially orally active antifungal agents such as ketoconazole, itraconazole, posaconazole, fluconazole and voriconazole. The chemistry, in vitro and in vivo antifungal activity, pharmacology, and clinical applications of these marketed conazoles has been described.

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References
1.
Fromtling R . Overview of medically important antifungal azole derivatives. Clin Microbiol Rev. 1988; 1(2):187-217. PMC: 358042. DOI: 10.1128/CMR.1.2.187. View

2.
Sansone-Parsons A, Krishna G, Calzetta A, Wexler D, Kantesaria B, Rosenberg M . Effect of a nutritional supplement on posaconazole pharmacokinetics following oral administration to healthy volunteers. Antimicrob Agents Chemother. 2006; 50(5):1881-3. PMC: 1472190. DOI: 10.1128/AAC.50.5.1881-1883.2006. View

3.
Talele T, Kulkarni V . Three-dimensional quantitative structure-activity relationship (QSAR) and receptor mapping of cytochrome P-450(14 alpha DM) inhibiting azole antifungal agents. J Chem Inf Comput Sci. 1999; 39(2):204-10. DOI: 10.1021/ci9800413. View

4.
Connolly P, Wheat J, Schnizlein-Bick C, Durkin M, Kohler S, Smedema M . Comparison of a new triazole antifungal agent, Schering 56592, with itraconazole and amphotericin B for treatment of histoplasmosis in immunocompetent mice. Antimicrob Agents Chemother. 1999; 43(2):322-8. PMC: 89071. DOI: 10.1128/AAC.43.2.322. View

5.
Hughes C, Beggs W . Action of fluconazole (UK-49,858) in relation to other systemic antifungal azoles. J Antimicrob Chemother. 1987; 19(2):171-4. DOI: 10.1093/jac/19.2.171. View