Abstract
Adenosine 5’-monophosphate (AMP) activated protein kinase (AMPK) is a highly conserved sensor of cellular energy. AMPK has been recognized as a key regulator of mammalian metabolic function and has emerged as an attractive target for the treatment of metabolic disorders, including obesity and type 2 diabetes. The synthesis and biological evaluation of novel 3-(4-oxothieno[2,3-d]pyrimidin-3(4H)-yl)propanoic acid derivatives as AMPK activators are described. The in vivo proof of principle for plasma glucose lowering effect is exemplified with a lead compound from this series.
Keywords: AMP-activated protein kinase (AMPK), AMPK activators, Thienopyrimidinone derivatives, Type-2 diabetes mellitus, db/db mice model.
Letters in Drug Design & Discovery
Title:Novel 4-Oxothienopyrimidinyl Propanoic Acid Derivatives as AMPActivated Protein Kinase (AMPK) Activators
Volume: 11 Issue: 6
Author(s): Chandrasekhar Abbineni, Saibal Kumar Das, Rashmi Talwar, Parimal Misra, Vijay Potluri, Menon C. A. Vinu, Thammera Ranjith Kumar, S. Sridhar, M. Roshaiah, Pradip K. Sasmal, P. Narasimha Rao, Khaji Abdul Rawoof, Poondla. Neelima, Nutakki Ravi Kumar, Megha Bhattacharya, M. Munikumar, P. Tirumala Rao and Mahaboobi Jaleel
Affiliation:
Keywords: AMP-activated protein kinase (AMPK), AMPK activators, Thienopyrimidinone derivatives, Type-2 diabetes mellitus, db/db mice model.
Abstract: Adenosine 5’-monophosphate (AMP) activated protein kinase (AMPK) is a highly conserved sensor of cellular energy. AMPK has been recognized as a key regulator of mammalian metabolic function and has emerged as an attractive target for the treatment of metabolic disorders, including obesity and type 2 diabetes. The synthesis and biological evaluation of novel 3-(4-oxothieno[2,3-d]pyrimidin-3(4H)-yl)propanoic acid derivatives as AMPK activators are described. The in vivo proof of principle for plasma glucose lowering effect is exemplified with a lead compound from this series.
Export Options
About this article
Cite this article as:
Abbineni Chandrasekhar, Das Kumar Saibal, Talwar Rashmi, Misra Parimal, Potluri Vijay, Vinu C. A. Menon, Kumar Ranjith Thammera, Sridhar S., Roshaiah M., Sasmal K. Pradip, Rao Narasimha P., Rawoof Abdul Khaji, Neelima Poondla., Kumar Ravi Nutakki, Bhattacharya Megha, Munikumar M., Rao Tirumala P. and Jaleel Mahaboobi, Novel 4-Oxothienopyrimidinyl Propanoic Acid Derivatives as AMPActivated Protein Kinase (AMPK) Activators, Letters in Drug Design & Discovery 2014; 11 (6) . https://dx.doi.org/10.2174/1570180811666140122003044
DOI https://dx.doi.org/10.2174/1570180811666140122003044 |
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
-
Targeting Established Tumor Vasculature: A Novel Approach to Cancer Treatment
Current Cancer Therapy Reviews Effect of Immunoglobulin Therapy on Blood Viscosity and potential concerns of Thromboembolism, Especially in Patients with Acute Kawasaki Disease
Recent Patents on Cardiovascular Drug Discovery Effect of GLP-1 Based Therapies on Diabetic Dyslipidemia
Current Diabetes Reviews Nitric Oxide-Mediated Endothelial Dysfunction - Is there Need to Treat?
Current Vascular Pharmacology Chronic Inflammatory Diseases: Progress and Prospect with Herbal Medicine
Current Pharmaceutical Design Caring for Children with Medical Complexity: Definitions, Challenges and Solutions
Current Pediatric Reviews The Pleiotropic Effects of ARB in Vascular Endothelial Progenitor Cells
Current Vascular Pharmacology A Glycemic Threshold of 90 mg/dl Promotes Early Signs of Atherosclerosis in Apparetly Healthy Overweight/Obese Subjects
Endocrine, Metabolic & Immune Disorders - Drug Targets Mediterranean Diet and Dementia of the Alzheimer Type
Current Aging Science Metabolic Homeostasis and Colonic Health: the Critical Role of Short Chain Fatty Acids
Current Nutrition & Food Science TNF as a Target of Inflammation in Rheumatoid Arthritis
Endocrine, Metabolic & Immune Disorders - Drug Targets 1h Post-load Blood Glucose in the Identification of Proatherogenic Cardiometabolic Profile in Obesity
Endocrine, Metabolic & Immune Disorders - Drug Targets Colchicine: A Review on Chemical Structure and Clinical Usage
Infectious Disorders - Drug Targets A Comparative Assessment of Metabolic Syndrome and its Association with Vitamin D and Other Risk Factors in Type 2 Diabetes Mellitus Patients
Current Diabetes Reviews Identify Compounds' Target Against Alzheimer's Disease Based on In-Silico Approach
Current Alzheimer Research The Role of Vitamin D in Dyslipidemia and Cardiovascular Disease
Current Pharmaceutical Design COPD Management: Look Beyond the Airway Obstruction, Chronic Bronchitis and Emphysema
Current Respiratory Medicine Reviews Antioxidative Effects of Rhodiola Genus: Phytochemistry and Pharmacological Mechanisms against the Diseases
Current Topics in Medicinal Chemistry Bergamot (Citrus bergamia Risso) Flavonoids and Their Potential Benefits in Human Hyperlipidemia and Atherosclerosis: an Overview
Mini-Reviews in Medicinal Chemistry Nitric Oxide Synthases and Their Natural Inhibitors
Current Enzyme Inhibition