McElroy, William T. published the artcilePotent and Selective Amidopyrazole Inhibitors of IRAK4 That Are Efficacious in a Rodent Model of Inflammation, Recommanded Product: tert-Butyl 4-(5-amino-1H-pyrazol-3-yl)piperidine-1-carboxylate, the main research area is preparation amidopyrazole inhibitor IRAK4 inflammation structure; Interleukin-1 receptor-associated kinase 4; SAR; drug discovery; inflammation; structure-based drug design.
IRAK4 is a critical upstream kinase in the IL-1R/TLR signaling pathway. Inhibition of IRAK4 is hypothesized to be beneficial in the treatment of autoimmune related disorders. A screening campaign identified a pyrazole class of IRAK4 inhibitors that were determined by X-ray crystallog. to exhibit an unusual binding mode. SAR efforts focused on the identification of a potent and selective inhibitor with good aqueous solubility and rodent pharmacokinetics. Pyrazole C-3 piperidines were well tolerated, with N-sulfonyl analogs generally having good rodent oral exposure but poor solubility N-Alkyl piperidines exhibited excellent solubility and reduced exposure. Pyrazoles possessing N-1 pyridine and fluorophenyl substituents were among the most active. Piperazine 32 was a potent enzyme inhibitor with good cellular activity. Compound 32 reduced the in vivo production of proinflammatory cytokines and was orally efficacious in a mouse antibody induced arthritis disease model of inflammation.
ACS Medicinal Chemistry Letters published new progress about Anti-inflammatory agents. 1169563-99-8 belongs to class pyrazoles-derivatives, name is tert-Butyl 4-(5-amino-1H-pyrazol-3-yl)piperidine-1-carboxylate, and the molecular formula is C13H22N4O2, Recommanded Product: tert-Butyl 4-(5-amino-1H-pyrazol-3-yl)piperidine-1-carboxylate.
Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics