双三唑衍生物UK 49,858与两性霉素B对荚膜组织胞浆菌的体外和体内活性比较。
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.
作者信息
Kobayashi G S, Travis S, Medoff G
出版信息
Antimicrob Agents Chemother. 1986 Apr;29(4):660-2. doi: 10.1128/AAC.29.4.660.
Abstract
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.
摘要
二氟苯基双三唑衍生物UK 49,858的抗真菌活性在体外针对7株荚膜组织胞浆菌进行了评估，并在荚膜组织胞浆菌病的AKR和C57BL/6小鼠模型中进行了体内评估。与两性霉素B相比，UK 49,858对AKR和C57BL/6小鼠的毒性更低。UK 49,858对AKR小鼠的治疗指数为4.3，对C57BL/6小鼠为7.1；两性霉素B对两种小鼠品系的治疗指数均为2。口服给药时，在感染荚膜组织胞浆菌的AKR或C57BL/6小鼠中，UK 49,858与腹腔注射两性霉素B相比效果良好。
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