The azoles are the prominent broad spectrum oral antifungal agents in use or under clinical investigation for the systemic mycoses. This class of antifungal agents is represented by the marketed drug ketoconazole (Nizoral) and the experimental triazoles furthest along in clinical trials in the Unite
The search for new triazole antifungal agents
โ Scribed by Yigal Koltin; Christopher A Hitchcock
- Book ID
- 104414899
- Publisher
- Elsevier Science
- Year
- 1997
- Tongue
- English
- Weight
- 932 KB
- Volume
- 1
- Category
- Article
- ISSN
- 1367-5931
No coin nor oath required. For personal study only.
โฆ Synopsis
The first generation antifungal agent triazoles, fluconazole and itraconazole, have revolutionised the treatment of serious fungal infections such as mucosal and invasive candidiasis and cryptococcal meningitis. However, the treatment of some fungal infections, particularly aspergillosis, is still far from satisfactory and thus there is an important requirement for new broad-spectrum antifungal agents. The new second generation triazoles voriconazole and SCH-56592 show considerable promise in achieving this goal in the near future.
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Previous studies implicated the cytochrome P450 (CYP) system as critical in the teratogenic bioactivation of phenytoin (PHT). Fluconazole (FCZ) is an antifungal bis-triazole with potent inhibitory effect on the principal CYP-dependent metabolic pathway of PHT. In this study an in vivo experimental m