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  • Title: Antimycotic imidazoles. part 4. Synthesis and antifungal activity of ketoconazole, a new potent orally active broad-spectrum antifungal agent.
    Author: Heeres J, Backx LJ, Mostmans JH, Van Cutsem J.
    Journal: J Med Chem; 1979 Aug; 22(8):1003-5. PubMed ID: 490531.
    Abstract:
    The preparation and antifungal properties of cis-1-acetyl-4-[4-[[2-(2,4-dichlorophenyl)-2-(1H-imidazol-1-yl-methyl)-1,3-dioxolan-4-yl]methoxy]phenyl]piperazine (I) are described. Ketoconazole has, at low oral doses, a high in vivi activity against vaginal candidosis in rats and against cutaneous candidosis in guinea pigs.
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