SDS of cas: 70298-88-3On September 10, 2009 ,《Design, Synthesis, and Structure-Activity Relationships of Aminopyridine N-Oxides, a Novel Scaffold for the Potent and Selective Inhibition of p38 Mitogen Activated Protein Kinase》 was published in Journal of Medicinal Chemistry. The article was written by Lumeras, Wenceslao; Caturla, Francisco; Vidal, Laura; Esteve, Cristina; Balague, Cristina; Orellana, Adelina; Dominguez, Maria; Roca, Ramon; Huerta, Josep M.; Godessart, Nuria; Vidal, Bernat. The article contains the following contents:
A novel series of aminopyridine N-oxides, e.g. I, were designed, synthesized, and tested for their ability to inhibit p38α MAP kinase. Some of these compounds showed a significant reduction in the LPS-induced TNFα production in human whole blood. Structure-activity relationship studies revealed that N-oxide oxygen was essential for activity and was probably a determinant factor for a marked selectivity against other related kinases. Compound I was identified as a potent and selective p38α inhibitor with an appropriate balance between potency and pharmacokinetics. In vivo efficacy of I was demonstrated in reducing TNFα levels in an acute murine model of inflammation (ED50 = 1 mg/kg in LPS-induced TNFα production when dosed orally 1.5 h prior to LPS administration). The oral efficacy of I was further demonstrated in a chronic model of adjuvant arthritis in rats with established disease when administered orally (ED50 = 4.5 mg/kg). The experimental process involved the reaction of 2,2-Dimehtyl-N-pyridin-3-yl-propionamide(cas: 70298-88-3SDS of cas: 70298-88-3)
2,2-Dimehtyl-N-pyridin-3-yl-propionamide(cas: 70298-88-3) belongs to anime. In organic chemistry, amines are compounds and functional groups that contain a basic nitrogen atom with a lone pair. Amines are formally derivatives of ammonia (NH3), wherein one or more hydrogen atoms have been replaced by a substituent such as an alkyl or aryl group (these may respectively be called alkylamines and arylamines; amines in which both types of substituent are attached to one nitrogen atom may be called alkylarylamines).SDS of cas: 70298-88-3
Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics