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Molecules 2010, 15(6), 4129-4188; doi:10.3390/molecules15064129


Leemskuilen 18, B-2350 Vosselaar, Belgium
Johnson & Johnson Pharmaceutical Research & Development, a division of Janssen Pharmaceutica N.V.,Turnhoutseweg 30, B-2340 Beerse, Belgium
Pater Van Mierlostraat 18, B-2300 Turnhout, Belgium
Author to whom correspondence should be addressed.
Received: 4 May 2010 / Accepted: 7 June 2010 / Published: 9 June 2010
(This article belongs to the Special Issue Anti-Infective Agents)
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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.
Keywords: miconazole; ketoconazole; itraconazole; posaconazole; fluconazole; voriconazole; antifungal miconazole; ketoconazole; itraconazole; posaconazole; fluconazole; voriconazole; antifungal

This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).

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Heeres, J.; Meerpoel, L.; Lewi, P. Conazoles. Molecules 2010, 15, 4129-4188.

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