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.
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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 |
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