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
-
New Technologies for the Diagnosis of Sleep Apnea
Current Hypertension Reviews Optimizing the Management of Uncontrolled/Resistant Hypertension. The Importance of Sleep Apnoea Syndrome
Current Vascular Pharmacology Vascular Pharmacotherapy and Dementia
Current Vascular Pharmacology Targeted Therapies in Solid Tumours: Pinpointing the Tumours Achilles Heel
Current Pharmaceutical Design Regular Physical Activity and Vascular Aging
Current Pharmaceutical Design Human Urotensin II and Metabolic Syndrome
Vascular Disease Prevention (Discontinued) Development of Calorie Restriction Mimetics as Therapeutics for Obesity, Diabetes, Inflammatory and Neurodegenerative Diseases
Current Genomics Hydroxyimine NO-Donors; FK409 and Derivatives
Current Topics in Medicinal Chemistry Reproductive Health Indicators and Factors Affecting Menstrual Cycle Pattern among Sudanese Women with Thyroid Dysfunction
Current Women`s Health Reviews Taurine Analogues; A New Class of Therapeutics: Retrospect and Prospects
Current Medicinal Chemistry The Saphenous Vein as a Bypass Conduit: The Potential Role of Vascular Nerves in Graft Performance
Current Vascular Pharmacology Metabolic Syndrome and Diabetic Atherothrombosis: Implications in Vascular Complications
Current Molecular Medicine Quercetin-Phospholipid Complex: An Amorphous Pharmaceutical System in Herbal Drug Delivery
Current Drug Discovery Technologies Assessment and Management of Volume Overload Among Patients on Chronic Dialysis
Current Vascular Pharmacology ROCK Inhibitors as Emerging Therapeutic Candidates for Sarcomas
Current Cancer Drug Targets Biomarkers Determining Cardiovascular Risk in Patients with Kidney Disease
Current Medicinal Chemistry Coronary Artery Ectasia-A Review of Current Literature
Current Cardiology Reviews Prevalence of HTN in Iran: Meta-analysis of Published Studies in 2004-2018
Current Hypertension Reviews Prothrombotic Potential of NSAID in Ischemic Heart Diesase
Mini-Reviews in Medicinal Chemistry Recent Advances in Antiarrhythmic Drug Treatment of Atrial Fibrillation
Recent Patents on Cardiovascular Drug Discovery