Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 20, Issue 22, Pages 6671-6675Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2010.09.012
Keywords
p38; MAP kinase; Pyridinylimidazoles; ATP competitive inhibitors
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The synthesis of 2,4,5-trisubstituted and 1,2,4,5-tetrasubstituted imidazoles as potent p38 alpha 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 p38 alpha MAP kinase inhibition assay. The structure-activity relationships between these two series are different and not comparable. (C) 2010 Elsevier Ltd. All rights reserved.
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