Issue 5, 2000
From the journal:

Journal of the Chemical Society, Perkin Transactions 1

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

Keith Biggadike,a   Sean M. Lynn,a   Panayiotis A. Procopiou,*a   Rupert E. Shawa  and  Christopher Williamsona  

* Corresponding authors

a Glaxo Wellcome Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire, UK

Abstract

A series of novel γ-butyrolactones fused at the 16β,17β position of the 9α-fluoro-11β-hydroxy-3-oxoandrosta-1,4-diene nucleus and possessing oxygen substituents at 16α,17α 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 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.

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Article information

DOI
https://doi.org/10.1039/A908358H
Article type
Paper
Submitted
19 Oct 1999
Accepted
21 Dec 1999
First published
16 Feb 2000

J. Chem. Soc., Perkin Trans. 1, 2000, 813-818

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

K. Biggadike, S. M. Lynn, P. A. Procopiou, R. E. Shaw and C. Williamson, J. Chem. Soc., Perkin Trans. 1, 2000, 813 DOI: 10.1039/A908358H

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