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Molecules 2010, 15(6), 4129-4188; doi:10.3390/molecules15064129
1 Leemskuilen 18, B-2350 Vosselaar, Belgium 2 Johnson & Johnson Pharmaceutical Research & Development, a division of Janssen Pharmaceutica N.V.,Turnhoutseweg 30, B-2340 Beerse, Belgium 3 Pater Van Mierlostraat 18, B-2300 Turnhout, Belgium
* Author to whom correspondence should be addressed.
Received: 4 May 2010; in revised form: / Accepted: 7 June 2010 / Published: 9 June 2010
(This article belongs to the Special Issue Anti-Infective Agents)
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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.
Keywords: miconazole; ketoconazole; itraconazole; posaconazole; fluconazole; voriconazole; antifungal
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MDPI and ACS Style
Heeres, J.; Meerpoel, L.; Lewi, P. Conazoles. Molecules 2010, 15, 4129-4188.AMA Style
Heeres J, Meerpoel L, Lewi P. Conazoles. Molecules. 2010; 15(6):4129-4188.Chicago/Turabian Style
Heeres, Jan; Meerpoel, Lieven; Lewi, Paul. 2010. "Conazoles." Molecules 15, no. 6: 4129-4188.