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Title: Tri- and tetrasubstituted imidazoles as p38α mitogen-activated protein kinase inhibitors. Author: Laufer S, Hauser D, Stegmiller T, Bracht C, Ruff K, Schattel V, Albrecht W, Koch P. Journal: Bioorg Med Chem Lett; 2010 Nov 15; 20(22):6671-5. PubMed ID: 20934337. Abstract: The synthesis of 2,4,5-trisubstituted and 1,2,4,5-tetrasubstituted imidazoles as potent p38α mitogen-activated protein kinase inhibitors is described. The trisubstituted imidazole series was found to be more potent than the tetrasubstituted imidazole series. Many of these compounds show low-nanomolar activities in the isolated p38α MAP kinase inhibition assay. The structure-activity relationships between these two series are different and not comparable.[Abstract] [Full Text] [Related] [New Search]