Comparison of the in vitro and in vivo activity of the bis-triazole derivative UK 49,858 with that of amphotericin B against Histoplasma capsulatum.
The antifungal activity of UK 49,858, a difluorophenyl bis-triazole derivative, was evaluated in vitro against seven strains of Histoplasma capsulatum and in vivo in AKR and C57BL/6 murine models of histoplasmosis. UK 49,858 had a lower toxicity for AKR and C57BL/6 mice than amphotericin B did. The therapeutic index of UK 49,858 was 4.3 for AKR mice and 7.1 for C57BL/6; with amphotericin B it was 2 for both mouse strains. Given orally, UK 49,858 compared favorably with amphotericin B given intraperitoneally in either AKR or C57BL/6 mice infected with H. capsulatum.
D000666:Amphotericin B / Q000494:pharmacology* / Q000627:therapeutic use; D000818:Animals; D015725:Fluconazole; D006658:Histoplasma / Q000187:drug effects*; D006660:Histoplasmosis / Q000188:drug therapy*; D066298:In Vitro Techniques; D051379:Mice; D008826:Microbial Sensitivity Tests; D014230:Triazoles / Q000494:pharmacology* / Q000627:therapeutic use
D014230:Triazoles; D000666:Amphotericin B; D015725:Fluconazole