Mirguet, Olivier; Sautet, Stephane; Clement, Catherine-Anne; Toum, Jerome; Donche, Frederic; Marques, Celine; Rondet, Emilie; Pizzonero, Mathieu; Beaufils, Benjamin; Dudit, Yann; Huet, Pascal; Trottet, Lionel; Grondin, Pascal; Brusq, Jean-Marie; Boursier, Eric; Saintillan, Yannick; Nicodeme, Edwige published the artcile< Discovery of Pyridones as Oral AMPK Direct Activators>, Recommanded Product: Ethyl 3-amino-1H-pyrrole-2-carboxylate, the main research area is pyridone AMPK activator diabetes type 2 structure activity preperation; AMPK direct activator; P-gp substrate; pyridone; type 2 diabetes.
AMP-activated protein kinase (AMPK) is an evolutionarily conserved fuel-sensing enzyme that is activated in shortage of energy and suppressed in its surfeit. AMPK activation stimulates fatty acid oxidation, enhances insulin sensitivity, alleviates hyperglycemia and hyperlipidemia, and inhibits proinflammatory changes. Thus, AMPK is a well-received therapeutic target for type 2 diabetes and other metabolic disorders. Here, the authors will report the discovery of pyrrolopyridone derivatives as AMPK direct activators. The authors will illustrate the synthesis and structure-activity relationships of the series as well as some pharmacokinetic results. Some compounds exhibited encouraging oral exposure and were evaluated in a mouse diabetic model. 2-Chloro-7-hydroxy-1-[2′-hydroxy-3′-(methyloxy)-4-biphenylyl]-6-phenyl-1,4-dihydro5H-pyrrolo[3,2-b]pyridin-5-one showed oral activity at 30 mg/kg on blood glucose.
ACS Medicinal Chemistry Letters published new progress about Drug discovery. 252932-48-2 belongs to class esters-buliding-blocks, and the molecular formula is C7H10N2O2, Recommanded Product: Ethyl 3-amino-1H-pyrrole-2-carboxylate.
Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics