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Letters in Drug Design & Discovery
ISSN (Print): 1570-1808
ISSN (Online): 1875-628X
Epub Full Text Article
DOI: 10.2174/1570180811666140122003044      Price:  $95

Novel 4-Oxothienopyrimidinyl Propanoic Acid Derivatives as AMP-activated Protein Kinase (AMPK) Activators

Author(s): Pradip K. Sasmal, Mahaboobi Jaleel, P. Tirumala Rao, M. Munikumar, Megha Bhattacharya, Nutakki Ravi Kumar, P. Neelima, Khaji Abdul Rawoof, P. Narasimha Rao, Chandrasekhar Abbineni, M. Roshaiah, S. Sridhar, Thammera Ranjith Kumar, Menon C. A. Vinu, Vijay Potluri, Parimal Misra, Rashmi Talwar and Saibal Kumar Das
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.
AMP-activated protein kinase (AMPK), AMPK activators, Thienopyrimidinone derivatives, Type-2 diabetes mellitus, db/db mice model
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