Name | (2R,3S)-2-(2,4-difluorophenyl)-3-(5-fluoro-4-pyrimidinyl)-1-(1H-1,2,4-triazol-1-yl)-2-butanol (1R)-10-camphorsulfonate |
---|---|
Synonyms |
voriconazole
[(1R,4S)-7,7-Dimethyl-2-oxobicyclo[2.2.1]hept-1-yl]methanesulfonic acid - (2R,3S)-2-(2,4-difluorophenyl)-3-(5-fluoro-4-pyrimidinyl)-1-(1H-1,2,4-triazol-1-yl)-2-butanol (1:1) Bicyclo[2.2.1]heptane-1-methanesulfonic acid, 7,7-dimethyl-2-oxo-, (1R,4S)-, compd. with (αR,βS)-α-(2,4-difluorophenyl)-5-fluoro-β-methyl-α-(1H-1,2,4-triazol-1-ylmethyl)-4-pyrimidine 
ethanol (1:1) voriconazole (1r)-(-)-10-camphorsulfonate (2r,3s)-2-(2,4-difluorophenyl)-3-(5-fluoropyrimidin-4-yl)-1-(1h-1,2,4-triazol-1-yl)butan-2-ol l(-)-camphorsulfonate (2r,3s)-2-(2,4-difluorophenyl)-3-(5-fluoropyrimidin-4-yl)-1-(1h-1,2,4-triazol-1-yl)butan-2-oll-(-)-10-camphorsulfonate |
Description | Voriconazole (UK-109496) camphorsulfonate is a second-generation, broad-spectrum triazole antifungal agent that inhibits fungal ergosterol biosynthesis. Voriconazole camphorsulfonate exerts its antifungal activity by inhibition of 14-α-lanosterol demethylation, which is mediated by fungal cytochrome P450 enzymes[1][2]. |
---|---|
Related Catalog | |
In Vitro | Voriconazole camphorsulfonate has great activity against S. apiospermum and C. neoformans with the MICs of 0.5 μg/mL and 0.125–0.25 μg/mL, respectively[1]. Voriconazole camphorsulfonate inhibits the cytochrome P450 (CYP)-dependent enzyme 14-alpha-sterol demethylase, thereby disrupting the cell membrane and halting fungal growth[2]. |
In Vivo | Voriconazole (5-20 mg/kg; p.o. for 21 days) camphorsulfonate prolongs survival in a dose-dependent fashion. Voriconazole (40 mg/kg/day) camphorsulfonate decreases the fungal burden in the lungs[3]. Animal Model: Male specific-pathogen-free BALB/cByJ mice[3] Dosage: 1, 5, 20 mg/kg/day Administration: P.o. once daily for 21 days Result: Improved survival in a dose-response fashion, with median survival times (MSTs) of 21, 28, and 35 days with doses of 1, 5, and 20 mg/kg, respectively. |
References |
Molecular Formula | C26H30F3N5O5S |
---|---|
Molecular Weight | 581.607 |
Exact Mass | 581.191956 |
PSA | 156.54000 |
LogP | 4.52730 |