Piperidine-based heterocyclic oxalyl amides as potent p38α MAP kinase inhibitors
2010
The design and synthesis of a new class of p38α MAP kinase inhibitors based on 4-fluorobenzylpiperidine heterocyclic oxalyl
amidesare described. Many of these compounds showed low-nanomolar activities in p38α enzymatic and cell-based cytokine TNFα
production inhibitionassays. The optimal linkers between the
piperidineand the oxalyl
amidewere found to be [6,5] fused ring heterocycles. Substituted indoles and azaindoles were favored
structural motifsin the cellular assay.
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