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
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:
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.
Export Options
About this article
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
DOI https://dx.doi.org/10.2174/1570180043485734 |
Print ISSN 1570-1808 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-628X |
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
Related Articles
-
Cardiovascular and Antidipsogenic Effects of Nesfatin-1
Current Pharmaceutical Design New Strategies in Treatment of Mineral and Bone Disorders and Associated Cardiovascular Disease in Patients with Chronic Kidney Disease
Recent Patents on Cardiovascular Drug Discovery Management of Measurable Variable Cardiovascular Disease' Risk Factors
Current Cardiology Reviews Cardioprotective Potential of Iron Chelators and Prochelators
Current Medicinal Chemistry Bariatric Surgery and it Effects on the Respiratory System
Current Respiratory Medicine Reviews Complex Inheritance for Susceptibility to Sudden Cardiac Death
Current Pharmaceutical Design Design, Synthesis and Biological Evaluation of Some Oxadiazole Derivatives as Novel Amide-Based Inhibitors of Soluble Epoxide Hydrolase
Letters in Drug Design & Discovery Blood Platelet Reactivity and its Pharmacological Modulation in (People with) Diabetes Mellitus
Current Pharmaceutical Design Hemothorax
Current Respiratory Medicine Reviews Drug Repositioning for Treatment of Movement Disorders: From Serendipity to Rational Discovery Strategies
Current Topics in Medicinal Chemistry Conivaptan: Potential Therapeutic Implications in Heart Failure
Recent Patents on Cardiovascular Drug Discovery Epigenetic Modulation of Myocardial Angiogenic Balance: An Emerging Therapeutic Perspective for Adult Failing Heart
Current Angiogenesis (Discontinued) Renal Injury Following Intravitreal Anti-VEGF Administration in Diabetic Patients with Proliferative Diabetic Retinopathy and Chronic Kidney Disease - A Possible Side Effect?
Current Drug Safety Imaging of Organ Metabolism in Obesity and Diabetes: Treatment Perspectives
Current Pharmaceutical Design Local Renin-Angiotensin II Systems, Angiotensin-Converting Enzyme and its Homologue ACE2: Their Potential Role in the Pathogenesis of Chronic Obstructive Pulmonary Diseases, Pulmonary Hypertension and Acute Respiratory Distress Syndrome
Current Medicinal Chemistry Mechanism of Cardiac Pathogenesis and Cardiotoxicity of Anti- COVID-19 Drugs
Coronaviruses Adverse Drug Reactions Related to Drug Administration in Hospitalized Patients
Current Drug Safety Molecular Targets for Promoting Wound Healing in Diabetes
Recent Patents on Endocrine, Metabolic & Immune Drug Discovery New Strategies and Drugs in the Treatment of Hypertension: Monotherapy or Combination?
Recent Patents on Cardiovascular Drug Discovery Depression, Antidepressants and Hypertensive Disorders of Pregnancy: A Systematic Review
Current Drug Safety