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Letters in Drug Design & Discovery

Editor-in-Chief

ISSN (Print): 1570-1808
ISSN (Online): 1875-628X

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

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

Volume 11, Issue 6, 2014

Page: [778 - 785] Pages: 8

DOI: 10.2174/1570180811666140122003044

Price: $65

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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