Novel glucocorticoid antedrugs possessing a C16,17-fused γ-lactone ring

被引：6

作者：

Biggadike, K ^{[1
]}

Lynn, SM ^{[1
]}

Procopiou, PA ^{[1
]}

Shaw, RE ^{[1
]}

Williamson, C ^{[1
]}

机构：

[1] Glaxo Wellcome Res & Dev Ltd, Med Res Ctr, Stevenage SG1 2NY, Herts, England

来源：

JOURNAL OF THE CHEMICAL SOCIETY-PERKIN TRANSACTIONS 1 | 2000年 / 05期

关键词：

D O I：

10.1039/a908358h

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

A series of novel gamma-butyrolactones fused at the 16 beta,17 beta position of the 9 alpha-fluoro-11 beta-hydroxy-3-oxoandrosta-1,4-diene nucleus and possessing oxygen substituents at 16 alpha,17 alpha positions were prepared and tested as glucocorticoid agonists. The compounds were also tested for their lability in human plasma. Lactone 5 was found to be rapidly hydrolysed in plasma, whereas derivative 18 dagger was found to be a potent glucocorticoid agonist, but was stable in plasma. The structure of the C21S diastereoisomer of compound 18 was confirmed by an X-ray diffraction study.

引用

页码：813 / 818

页数：6

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