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Isaconazole is a novel extended spectrum triazole compound, which has activity against yeast, mold and dimorphic fungi and inhibits cytochrome P450 (CYP) - dependent 14 α- Lanosterol demethylation can inhibit the synthesis of ergosterol in fungal cell membrane.
Synonymous | 4-[2-[(2R,3R)-3-(2,5-difluorophenyl)-3-hydroxy-4-(1,2,4-triazol-1-yl)butan-2-yl]-1,3-thiazol-4-yl]benzonitrile;;4-(2-((2R,3R)-3-(2,5-difluorophenyl)-3-hydroxy-4-(1H-1,2,4-triazol-1-yl)butan-2-yl)thiazol-4-yl)benzonitrile |
Structure |
|
CAS | 241479-67-4 |
Molecular Formula | C22H17F2N5OS |
Molecular Weight | 437.47 |
Appearance | White powder |
Packing | 25kg cardboard barrel |
Uses | Triazole antifungal drugs |
Storage | Sealed in dry,2-8°C |
After entering the body, isaconazole sulfate is rapidly transformed into the active metabolite isaconazole by Plasma Esterase. Similar to other azole antifungal drugs, isaconazole destroys the formation of fungal cell membrane by inhibiting ergosterol biosynthesis. Isaconazole and cytochrome P450 wool sterol 14 encoded by fungal CYP51 gene- α- Demethylase binding, inhibition 14- α- Demethylase activity hinders ergosterol synthesis, while the accumulated toxic methylated sterols affect the structural stability and integrity of fungal cell membrane, change its function, and eventually lead to fungal death. The side chain in the structural formula of isaconazole has high affinity with fungal CYP51 protein, which makes it have a wide antifungal spectrum, including fungi resistant to other azole antifungal drugs.
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