(2S,3R)-2-(2,4-ジフルオロフェニル)-3-(5-フルオロピリミジン-4-イル)-1-(1H-1,2,4-トリアゾール-1-イル)ブタン-2-オール 化学特性,用途語,生産方法
説明
Voriconazole-d3 is an Ergosterol biosynthesis inhibitor and a labeled form of Voriconazole. This mono triazole antifungal agent inhibits the growth of Candida, Cryptococcus, and Aspergillus species. Studies suggest that Voriconazole-d3 can be synthesized by modifying the structure of fluconazole. This antifungal agent functions by inhibiting cytochrome P450 dependent 14-α-sterol demethylase, which is responsible for the biosynthesis of Ergosterol. Furthermore, Voriconazole-d3 inhibits fungal growth, cell wall thinning, and cell membrane degradation.
使用
Voriconazole is a triazole antifungal agent used primarily in the treatment or prevention of aspergillosis and candidal infections. However, its therapy may cause transient, asymptomatic serum aminotransferase elevations, and it is also a well-known cause of acute drug-induced liver injury.
主な応用
Voriconazole-d3 is derived from 2,4-Difluoro-α-(1H-1,2,4-triazolyl)acetophenone, which is an antifungal activity, particularly toward Candida albicans and Candida parapsilosis.
参考文献
1. Voriconazole (UK-109,496) inhibits the growth and alters the morphology of fluconazole-susceptible and -resistant Candida species DOI:
10.1128/AAC.41.8.1840Belanger, P., et al. 1997. Antimicrob. Agents Chemother. 41: 1840-1842. PMID:
92577762. In vitro activities of voriconazole (UK-109,496) and four other antifungal agents against 394 clinical isolates of Candida spp
Marco, F., et al. 1998. Antimicrob. Agents Chemother. 42: 161-163. PMID:
94492783. In vitro activity of the new triazole voriconazole (UK-109,496) against opportunistic filamentous and dimorphic fungi and common and emerging yeast pathogens
Espinel-Ingroff, A. 1998. J. Clin. Microbiol. 36: 198-202. PMID:
9431946
(2S,3R)-2-(2,4-ジフルオロフェニル)-3-(5-フルオロピリミジン-4-イル)-1-(1H-1,2,4-トリアゾール-1-イル)ブタン-2-オール 上流と下流の製品情報
原材料
準備製品