Discovery of Potent, Non-Steroidal and Highly Selective Glucocorticoid Receptor Antagonists with Anti-Obesity Activity

1 January 2004

journal article
Published by Bentham Science Publishers Ltd. in Letters in Drug Design & Discovery

Vol. 1 (1) , 1-5
https://doi.org/10.2174/1570180043485734

Abstract

To thwart phase II metabolism, Structure-Activity-Relationship (SAR) studies around the phenol of the potent glucocorticoid receptor (GR) antagonists CP-394531 and CP-409069 were examined. The discovery of the potent, selective, nonsteroidal GR antagonist (CP-472555) with anti-GR and anti-obesity activity in animal models is described.

Keywords

NON-STEROIDAL
GLUCOCORTICOID
ANTAGONIST
ANTI-OBESITY

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