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含吗啉环的新型唑类衍生物UR-9746和UR-9751的体外抗真菌活性及其与氟康唑的比较。

In vitro antifungal activity of novel azole derivatives with a morpholine ring, UR-9746 and UR-9751, and comparison with fluconazole.

作者信息

Stevens D A, Aristizabal B H

机构信息

Department of Medicine, Santa Clara Valley Medical Center, San Jose, CA 95128-2699, USA.

出版信息

Diagn Microbiol Infect Dis. 1997 Oct;29(2):103-6. doi: 10.1016/s0732-8893(97)00104-1.

Abstract

Thirty-three patient fungal isolates were studied by broth macrodilution methods for susceptibility to novel azole derivatives with a morpholine ring, UR-9746 and UR-9751, and fluconazole. MICs (micrograms/ml) ranged widely, but none had lower MICs for Candida albicans or Cryptococcus neoformans than UR-9751. Fluconazole and UR-9751 had the most activity versus other Candida species. Activity was demonstrated versus endemic fungal pathogens. Aspergillus species were generally resistant, although modest activity was seen. UR-9746 and UR-9751 are active in vitro, with a potency comparable to that of fluconazole.

摘要

采用肉汤稀释法对33株患者真菌分离株进行研究,以检测其对含吗啉环的新型唑类衍生物UR-9746和UR-9751以及氟康唑的敏感性。最低抑菌浓度(μg/ml)范围广泛,但对于白色念珠菌或新型隐球菌,没有一种的最低抑菌浓度低于UR-9751。氟康唑和UR-9751对其他念珠菌属的活性最强。对地方性真菌病原体也有活性。曲霉菌属通常耐药,尽管可见一定活性。UR-9746和UR-9751在体外具有活性,其效力与氟康唑相当。

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