Illig, Carl R.; Manthey, Carl L.; Meegalla, Sanath K.; Wall, Mark J.; Chen, Jinsheng; Wilson, Kenneth J.; DesJarlais, Renee L.; Ballentine, Shelley K.; Schubert, Carsten; Crysler, Carl S.; Chen, Yanmin; Molloy, Christopher J.; Chaikin, Margery A.; Donatelli, Robert R.; Yurkow, Edward; Zhou, Zhao; Player, Mark R.; Tomczuk, Bruce E. published the artcile< Enhancement of kinase selectivity in a potent class of arylamide FMS inhibitors>, Application of C19H34O2, the main research area is arylamide preparation FMS kinase inhibitor; Anti-inflammatory; Colony-stimulating factor-1 receptor; FMS; Hypocellularity; KIT; Macrophage colony-stimulating factor; Rheumatoid arthritis.
Structure-activity relationship (SAR) studies on a highly potent series of arylamide FMS inhibitors were carried out with the aim of improving FMS kinase selectivity, particularly over KIT. Potent compound I [R = 4-(HOCH2CH2)piperazin-1-yl] (FMS IC50 0.7 nM, FMS cell IC50 6.1 nM) was discovered that had good PK properties and a greater than fivefold improvement in selectivity for FMS over KIT kinase in a cellular assay relative to the previously reported clin. candidate 4. This improved selectivity was manifested in vivo by no observed decrease in circulating reticulocytes, a measure of bone safety, at the highest studied dose. Compound I [R = 4-(HOCH2CH2)piperazin-1-yl] was highly active in a mouse pharmacodynamic model and demonstrated disease-modifying effects in a dose-dependent manner in a strep cell wall-induced arthritis model of rheumatoid arthritis in rats.
Bioorganic & Medicinal Chemistry Letters published new progress about Antirheumatic agents. 112-63-0 belongs to class esters-buliding-blocks, and the molecular formula is C19H34O2, Application of C19H34O2.
Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics