Piperidine-based heterocyclic oxalyl amides as potent p38α MAP kinase inhibitors

…, D Kizer, S Dugar, S Chakravarty, Y Xu, J Jung…

Index: Mavunkel, Babu J.; Perumattam, John J.; Tan, Xuefei; Luedtke, Gregory R.; Lu, Qing; Lim, Don; Kizer, Darin; Dugar, Sundeep; Chakravarty, Sarvajit; Xu, Yong-jin; Jung, Joon; Liclican, Albert; Levy, Daniel E.; Tabora, Jocelyn Bioorganic and Medicinal Chemistry Letters, 2010 , vol. 20, # 3 p. 1059 - 1062

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Citation Number: 13

Abstract

The design and synthesis of a new class of p38α MAP kinase inhibitors based on 4- fluorobenzylpiperidine heterocyclic oxalyl amides are described. Many of these compounds showed low-nanomolar activities in p38α enzymatic and cell-based cytokine TNFα production inhibition assays. The optimal linkers between the piperidine and the oxalyl amide were found to be [6, 5] fused ring heterocycles. Substituted indoles and azaindoles ...