Ottosen, Erik Rytter published the artcileSynthesis and structure-activity relationship of aminobenzophenones. A novel class of p38 MAP kinase inhibitors with high antiinflammatory activity, HPLC of Formula: 452-63-1, the main research area is aminobenzophenone preparation structure activity MAP kinase inhibitor antiinflammatory; skin inflammation aminobenzophenone preparation structure activity MAP kinase inhibitor; dermatitis aminobenzophenone preparation structure activity MAP kinase inhibitor antiinflammatory; human aminobenzophenone preparation structure activity MAP kinase inhibitor antiinflammatory; kinase phosphorylating MAP inhibitor aminobenzophenone preparation structure activity; tumor necrosis factor kinase MAP inhibitor aminobenzophenone preparation; interleukin tumor necrosis factor kinase MAP inhibitor aminobenzophenone preparation; inflammation inhibitor aminobenzophenone preparation structure activity p38 MAP kinase.
The synthesis and structure-activity relationship (SAR) of a series of 4-aminobenzophenones, as a novel compound class with high antiinflammatory activity, was reported. The initial lead, [4-[(2-aminophenyl)amino]phenyl](phenyl)methanone, was systematically optimized and resulted in compounds that potently inhibited the release of the proinflammatory cytokines IL-1β and TNF-α in human peripheral blood mononuclear cells stimulated by LPS. One of the most potent compounds, among others, was [4-[(2-aminophenyl)amino]-2-chlorophenyl](2-methylphenyl)methanone (I) with IC50 values of 14 and 6 nM for the inhibition of IL-1β and TNF-α, resp. Furthermore, these types of compounds were found to be potent and selective p38 MAP kinase inhibitors, e.g. I had an IC50 value of 10 nM. Mol. modeling was used to rationalize our SAR data and to propose a model for the interaction of I with the p38 MAP kinase. The model involved a favorable hydrogen bond between the carbonyl group of the benzophenone and the NH of Met-109, positioning ring A in the hydrophobic pocket I of the enzyme. Good antiinflammatory effects were demonstrated in two murine models of dermatitis after topical application (oxazolone and TPA model).
Journal of Medicinal Chemistry published new progress about Anti-inflammatory agents. 452-63-1 belongs to class bromides-buliding-blocks, name is 1-Bromo-4-fluoro-2-methylbenzene, and the molecular formula is C7H6BrF, HPLC of Formula: 452-63-1.
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary