Structure-Based Design, Synthesis, and Biological Evaluation of Imidazo[4,5-b]Pyridin-2-one-Based p38 MAP Kinase Inhibitors: Part 2 was written by Kaieda, Akira;Takahashi, Masashi;Fukuda, Hiromi;Okamoto, Rei;Morimoto, Shinji;Gotoh, Masayuki;Miyazaki, Takahiro;Hori, Yuri;Unno, Satoko;Kawamoto, Tomohiro;Tanaka, Toshimasa;Itono, Sachiko;Takagi, Terufumi;Sugimoto, Hiroshi;Okada, Kengo;Lane, Weston;Sang, Bi-Ching;Saikatendu, Kumar;Matsunaga, Shinichiro;Miwatashi, Seiji. And the article was included in ChemMedChem in 2019.Product Details of 29421-99-6 This article mentions the following:
We identified novel potent inhibitors of p38 mitogen-activated protein (MAP) kinase using a structure-based design strategy, beginning with lead compound, 3-(butan-2-yl)-6-(2,4-difluoroanilino)-1,3-dihydro-2H-imidazo[4,5-b]pyridin-2-one (1). To enhance the inhibitory activity of 1 against production of tumor necrosis factor-濞?(TNF-濞? in human whole blood (hWB) cell assays, we designed and synthesized hybrid compounds in which the imidazo[4,5-b]pyridin-2-one core was successfully linked with the p-methylbenzamide fragment. Among the compounds evaluated, 3-(3-tert-butyl-2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridin-6-yl)-4-methyl-N-(1-methyl-1H-pyrazol-3-yl)benzamide (25) exhibited potent p38 inhibition, superior suppression of TNF-濞?production in hWB cells, and also significant in vivo efficacy in a rat model of collagen-induced arthritis (CIA). In this paper, we report the discovery of potent, selective, and orally bioavailable imidazo[4,5-b]pyridin-2-one-based p38 MAP kinase inhibitors. In the experiment, the researchers used many compounds, for example, 4-Bromo-5-methylthiophene-2-carboxylic acid (cas: 29421-99-6Product Details of 29421-99-6).
4-Bromo-5-methylthiophene-2-carboxylic acid (cas: 29421-99-6) belongs to organobromine compounds. Bromo compounds are employed in a variety of metal-catalyzed coupling reactions. They are also ideal candidates for the synthesis of Grignard reagents that have wide-applicability in organic synthesis. alpha-Bromoesters are employed in the Reformatsky reaction for the synthesis of beta-hydroxyesters. The principal reactions for organobromides include dehydrobromination, Grignard reactions, reductive coupling, and nucleophilic substitution.Product Details of 29421-99-6
Referemce:
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bromide – Wiktionary