新型咪唑衍生物SM - 4470对实验性真菌感染的活性
Activity of SM-4470, a new imidazole derivative, against experimental fungal infections.
作者信息
Ichise K, Tanio T, Saji I, Okuda T
出版信息
Antimicrob Agents Chemother. 1986 Sep;30(3):366-9. doi: 10.1128/AAC.30.3.366.
The antifungal activity of orally active SM-4470, (R)-3-(n-butylthio)-2-(2,4-dichlorophenyl)-1-(imidazole-1-yl)-2-propanol hydrochloride, was compared with that of ketoconazole. SM-4470 showed twofold-higher activity than ketoconazole in the oral treatment of systemic infection with Candida albicans in mice. In addition, SM-4470 was effective against aspergillosis in mice, but ketoconazole was ineffective. The efficacy of SM-4470 was similar to that of ketoconazole in curing experimental candidal vaginitis in rats and trichophytosis in guinea pigs, although its serum concentrations in these animals were lower than those of ketoconazole. These data suggest that SM-4470 may be of value in the treatment of both systemic and superficial fungal infections in humans.
将口服活性药物SM-4470（(R)-3-(正丁硫基)-2-(2,4-二氯苯基)-1-(咪唑-1-基)-2-丙醇盐酸盐）的抗真菌活性与酮康唑进行了比较。在小鼠白色念珠菌全身性感染的口服治疗中，SM-4470的活性比酮康唑高两倍。此外，SM-4470对小鼠曲霉菌病有效，但酮康唑无效。在治愈大鼠实验性念珠菌性阴道炎和豚鼠皮肤癣菌病方面，SM-4470的疗效与酮康唑相似，尽管其在这些动物体内的血清浓度低于酮康唑。这些数据表明，SM-4470在治疗人类全身性和浅表性真菌感染方面可能具有价值。
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