Ramurthy, Savithri published the artcileDiscovery and optimization of novel pyridines as highly potent and selective glycogen synthase kinase 3 inhibitors, Computed Properties of 371-99-3, the publication is Bioorganic & Medicinal Chemistry Letters (2020), 30(4), 126930, database is CAplus and MEDLINE.
Glycogen synthase kinase-3 plays an essential role in multiple biochem. pathways in the cell, particularly in regards to energy regulation. As such, Glycogen synthase kinase-3 is an attractive target for pharmacol. intervention in a variety of disease states, particularly non-insulin dependent diabetes mellitus. However, due to homol. with other crucial kinases, such as the cyclin-dependent protein kinase CDC2, developing compounds that are both potent and selective is challenging. A novel series of derivatives of 5-nitro-N2-(2-(pyridine-2-ylamino)ethyl)pyridine-2,6-diamine were synthesized and potently inhibit glycogen synthase kinase-3 (GSK3). Potency in the low nanomolar range was obtained along with remarkable selectivity. The compounds activate glycogen synthase in insulin receptor-expressing CHO-IR cells and in primary rat hepatocytes, and have acceptable pharmacokinetics and pharmacodynamics to allow for oral dosing. The x-ray co-crystal structure of human GSK3-β in complex with compound 1-(6-((2-((6-amino-5-nitropyridin-2-yl)amino)ethyl)amino)-2-(2,4-dichlorophenyl)pyridin-3-yl)-4-methylpiperazin-2-one is reported and provides insights into the structural determinants of the series responsible for its potency and selectivity.
Bioorganic & Medicinal Chemistry Letters published new progress about 371-99-3. 371-99-3 belongs to alcohols-buliding-blocks, auxiliary class Trifluoromethylated Building Blocks, name is 2-((2,2,2-Trifluoroethyl)amino)ethanol, and the molecular formula is C4H8F3NO, Computed Properties of 371-99-3.
Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts