Structural optimization of 2-(2-aminopyridin-4-yl)-N-(3-carbamoyl-1H-pyrazol-4-yl)-1,3-oxazole-4-carboxamide derivatives as potent interleukin-1 receptor-associated kinase 4 inhibitors. (PubMed, Bioorg Med Chem) - Sep 15, 2026 - "In our efforts to enhance the IRAK4 inhibitory activity of AS2444697 (2) derivatives reported in our previous studies, a structure-activity relationship study on 1-methyl-1H-pyrazole analogs of 2 was conducted...The representative compounds 47 and 35, bearing cyclopropyl and 2,2,2-trifluoroethyl groups, respectively, exhibited considerably higher inhibition of IL-1β-stimulated IL-6 production in cellular assays than 2. Further, they also demonstrated improved selectivity for IL-1β signaling over tumor necrosis factor-α signaling compared with 2."
Journal • Immunology • Oncology • CYP1A2 • IL1B • IL6 • IRAK4 • TNFA
|
|
Emiko Imamura; Hiroshi Inami; Hiroyuki Usuda; Hisashi Hayashida; Junko Watanabe; Naohiro Aoyama; Takeshi Ishikawa; Tomonori Ito; Tsuyoshi Mizutani
|