Novel 4-Oxothienopyrimidinyl Propanoic Acid Derivatives as AMPActivated Protein Kinase (AMPK) Activators
Pradip K. Sasmal,
P. Tirumala Rao,
Nutakki Ravi Kumar,
Khaji Abdul Rawoof,
P. Narasimha Rao,
Thammera Ranjith Kumar,
Menon C. A. Vinu,
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.
Keywords: AMP-activated protein kinase (AMPK), AMPK activators, Thienopyrimidinone derivatives, Type-2 diabetes mellitus,
db/db mice model.
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