DESIGN AND SYNTHESIS OF 14-ALPHA-METHYL-15-AZA-D-HOMOSTEROLS AS NOVEL ANTIMYCOTICS

被引：41

作者：

DOLLE, RE

ALLAUDEEN, HS

KRUSE, LI

机构：

[1] Department of Immunology, Research and Development Division, Swedeland, PA 19479, Smith Kline & French

[2] Department of Medicinal Chemistry, Smith Kline & French Research Limited, Hertfordshire, AL6 9AR, Frythe, Welwyn

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 1990年 / 33卷 / 02期

关键词：

D O I：

10.1021/jm00164a065

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A novel series of 14α-methyl-15-aza-D-homosterols 3-7 has been synthesized. These compounds display significant antimycotic activity in vitro (MIC = 0.8-3.1 µg/mL) that compares quite favorably to the activity observed for fluconazole (MIC = 0.8 µg/mL). Azasterols 3 and 4 were active in vivo as reflected in the increased survival time of Candida albicans infected mice. The antimycotic activity of 3-7 is hypothesized to be a consequence of the inhibition of fungal 14,15-sterol reductase. © 1990, American Chemical Society. All rights reserved.

引用

页码：877 / 880

页数：4

共 29 条

[1] SOME BIOLOGICAL TRANSFORMATIONS INVOLVING UNSATURATED LINKAGES - IMPORTANCE OF CHARGE SEPARATION AND CHARGE NEUTRALIZATION IN ENZYME CATALYSIS [J].