SAR of 2,6-diamino-3,5-difluoropyridinyl substituted heterocycles as novel p38 MAP kinase inhibitors

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Abstract

2,6-Diamino-3,5-difluoropyridinyl substituted pyridinylimidazoles, -pyrroles, -oxazoles, -thiazoles and -triazoles have been identified as novel p38α inhibitors. Pyridinylimidazole 11 potently inhibited LPS-induced TNFα in mice, showed good efficacy in the established rat adjuvant (ED50: 10 mg/kg po b.i.d.) and collagen induced arthritis (ED50: 5 mg/kg po b.i.d.) with disease modifying properties based on histological analysis of the joints. © 2002 Published by Elsevier Science Ltd.

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Revesz, L., Di Padova, F. E., Buhl, T., Feifel, R., Gram, H., Hiestand, P., … Zimmerlin, A. G. (2002). SAR of 2,6-diamino-3,5-difluoropyridinyl substituted heterocycles as novel p38 MAP kinase inhibitors. Bioorganic and Medicinal Chemistry Letters, 12(16), 2109–2112. https://doi.org/10.1016/S0960-894X(02)00336-0

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