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
-
Stress and the α7 Nicotinic Acetylcholine Receptor
Current Drug Targets Different Patterns of Statin Use in Patients with Acute Myocardial Infarction
Current Vascular Pharmacology Fructose Consumption, Lipid Metabolism and the Metabolic Syndrome
Current Nutrition & Food Science Physiology, Pharmacology and Pathophysiology of the pH Regulatory Transport Proteins NHE1 and NBCn1: Similarities, Differences, and Implications for Cancer Therapy
Current Pharmaceutical Design Glycemic Variability, Oxidative Stress, and Impact on Complications Related to Type 2 Diabetes Mellitus
Current Diabetes Reviews Health Benefits of Manuka Honey as an Essential Constituent for Tissue Regeneration
Current Drug Metabolism Glaucoma Pathogenesis and Neurotrophins: Focus on the Molecular and Genetic Basis for Therapeutic Prospects
Current Neuropharmacology Advances in Adjuvant Therapy Against Acute Bacterial Meningitis
Current Drug Targets - Infectious Disorders Editorial (Thematic Issue: Pharmacologic Strategies with Afterload Reduction in Low Cardiac Output Syndrome After Pediatric Cardiac Surgery)
Current Vascular Pharmacology Estrogens Acting as Cardiovascular Agents: Direct Vascular Actions
Current Medicinal Chemistry - Cardiovascular & Hematological Agents Human Ghrelin: A Gastric Hormone with Cardiovascular Properties
Current Pharmaceutical Design The Role of PPARs in Obesity and other Insulin Resistance Associated Disorders
Current Medicinal Chemistry - Immunology, Endocrine & Metabolic Agents Safety of Dabigatran in an Elderly Population: Single Center Experience in Italy
Current Drug Safety Insulin, Thrombin, ERK1/2 Kinase and Vascular Smooth Muscle Cells Proliferation
Current Pharmaceutical Design Proteomics to Unravel Platelet-Related Diseases and Identify Novel Anti-Platelet Drugs
Current Medicinal Chemistry Sonoelastography for Pelvic Metastatic Malignant Pheochromocytoma: A Case Report
Current Medical Imaging Management of Antineutrophil Cytoplasmic Antibody Associated Vasculitis
Current Immunology Reviews (Discontinued) Drugs for the Treatment of Hypercholesterolemia and their Benefits Beyond Cholesterol Lowering to Prevent Vascular Disease
Vascular Disease Prevention (Discontinued) The Impact of Pharmaceutical Care Practice on the Practitioner and the Patient in the Ambulatory Practice Setting: Twenty-five Years of Experience
Current Pharmaceutical Design Alzheimer’s Disease and Environmental Exposure to Lead: The Epidemiologic Evidence and Potential Role of Epigenetics
Current Alzheimer Research