Conazoles.
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.
Heeres
Jan
J
Leemskuilen 18, B-2350 Vosselaar, Belgium. jan@heeres.be
Meerpoel
Lieven
L
Lewi
Paul
P
D000935:Antifungal Agents / Q000737:chemistry* / Q000494:pharmacology*; D015725:Fluconazole / Q000737:chemistry / Q000494:pharmacology; D017964:Itraconazole / Q000737:chemistry / Q000494:pharmacology; D007654:Ketoconazole / Q000737:chemistry / Q000494:pharmacology; D008825:Miconazole / Q000737:chemistry / Q000494:pharmacology; D015394:Molecular Structure; D011743:Pyrimidines / Q000737:chemistry / Q000494:pharmacology; D013329:Structure-Activity Relationship; D014230:Triazoles / Q000737:chemistry / Q000494:pharmacology; D065819:Voriconazole
D000935:Antifungal Agents; D011743:Pyrimidines; D014230:Triazoles; D017964:Itraconazole; C101425:posaconazole; D008825:Miconazole; D015725:Fluconazole; D065819:Voriconazole; D007654:Ketoconazole