Pfefferkorn, Jeffrey A.; Lou, Jihong; Minich, Martha L.; Filipski, Kevin J.; He, Mingying; Zhou, Ru; Ahmed, Syed; Benbow, John; Perez, Angel-Guzman; Tu, Meihua; Litchfield, John; Sharma, Raman; Metzler, Karen; Bourbonais, Francis; Huang, Cong; Beebe, David A.; Oates, Peter J. published the artcile< Pyridones as glucokinase activators: Identification of a unique metabolic liability of the 4-sulfonyl-2-pyridone heterocycle>, Name: 4,5-Dichloropyridin-2-amine, the main research area is aminopicoline carboxylic acid cyclization transamidation; sulfonyl pyridone preparation glucokinase activation antidiabetic human.
A promising area of novel anti-diabetic therapy involves identification of small mol. activators of the glucokinase enzyme to reduce blood glucose and normalize glucose stimulated insulin secretion. Herein, the identification and optimization of a series of 4-sulfonyl-2-pyridone, i.e. I, activators is reported. The activators were evaluated for in vitro biochem. activation and pharmacokinetic properties. As part of these efforts, a unique metabolic liability of the 4-sulfonyl-2-pyridone ring system was identified wherein this heterocycle readily undergoes conjugation with glutathione under non-enzymic conditions.
Bioorganic & Medicinal Chemistry Letters published new progress about Antidiabetic agents. 188577-68-6 belongs to class pyridine-derivatives, and the molecular formula is C5H4Cl2N2, Name: 4,5-Dichloropyridin-2-amine.