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

[ Vol. 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   Pages 778 - 785 ( 8 )

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.

Affiliation:

, Dr. Reddy's Laboratories Ltd., Proprietary Products, Innovation Plaza, Bachupally, Hyderabad 500090, India.

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