Conazoles

Molecules

Jan Heeres¹  Lieven Meerpoel¹ 

[1] ¹Leemskuilen 18, B-2350 Vosselaar, Belgium ²Johnson & Johnson Pharmaceutical Research & Development, a division of Janssen Pharmaceutica N.V.,Turnhoutseweg 30, B-2340 Beerse, Belgium ³Pater Van Mierlostraat 18, B-2300 Turnhout, Belgium

关键词: miconazole;    ketoconazole;    itraconazole;    posaconazole;    fluconazole;    voriconazole;    antifungal;   

DOI  :  10.3390/molecules15064129

来源: mdpi

【 摘 要 】

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.

【 授权许可】

CC BY   
This is an open access article distributed under the Creative Commons Attribution License (CC BY) which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.