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

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

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

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, Graeme F. Woodworth

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Journal Name: Letters in Drug Design & Discovery

Volume 1 , Issue 1 , 2004

DOI : 10.2174/1570180043485734

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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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Letters in Drug Design & Discovery

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:Pfizer Global Research and Development, Pfizer Inc., Groton, Connecticut 06340, USA.

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.

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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, “ Discovery of Potent, Non-Steroidal and Highly Selective Glucocorticoid Receptor Antagonists with Anti-Obesity Activity”, Letters in Drug Design & Discovery (2004) 1: 1. https://doi.org/10.2174/1570180043485734

DOI https://doi.org/10.2174/1570180043485734	Print ISSN 1570-1808
Publisher Name Bentham Science Publisher	Online ISSN 1875-628X

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VOLUME: 1
ISSUE: 1
Year: 2004

Page: [1 - 5]
Pages: 5
DOI: 10.2174/1570180043485734

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