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

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

Volume: 1 Issue: 1

Author(s): Bradley P. Morgan, Kevin K.-C. Liu, Deepak K. Dalvie, Andrew G. Swick, Diane M. Hargrove, Theresa C. Wilson, Janet A. LaFlamme, Melinda S. Moynihan, Margaret A. Rushing and Graeme F. Woodworth

Affiliation:

Keywords: non-steroidal, glucocorticoid, antagonist, anti-obesity

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.

Cite this article as:

Morgan P. Bradley, Liu K.-C. Kevin, Dalvie K. Deepak, Swick G. Andrew, Hargrove M. Diane, Wilson C. Theresa, LaFlamme A. Janet, Moynihan S. Melinda, Rushing A. Margaret and Woodworth F. Graeme, Discovery of Potent, Non-Steroidal and Highly Selective Glucocorticoid Receptor Antagonists with Anti-Obesity Activity, Letters in Drug Design & Discovery 2004; 1 (1) . https://dx.doi.org/10.2174/1570180043485734