Letters in Drug Design & Discovery

G. Perry
University of Texas
San Antonio, TX
Email: lddd@benthamscience.org


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

Author(s): Pradip K. Sasmal, Mahaboobi Jaleel, P. Tirumala Rao, M. Munikumar, Megha Bhattacharya, Nutakki Ravi Kumar, Poondla. 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, Saibal Kumar Das.

Graphical 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.

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Article Details

Year: 2014
Page: [778 - 785]
Pages: 8
DOI: 10.2174/1570180811666140122003044
Price: $58