期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 12, 期 16, 页码 2109-2112出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/S0960-894X(02)00336-0
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2,6-Diamino-3,5-difluoropyridinyl substituted pyridinylimidazoles, -pyrroles, -oxazoles, -thiazoles and -triazoles have been identified as novel p38alpha inhibitors. Pyridinylimidazole 11 potently inhibited LPS-induced TNFalpha in mice, showed good efficacy in the established rat adjuvant (ED50: 10mg/kg po b.i.d.) and collagen induced arthritis (ED50: 5mg/kg po b.i.d.) with disease modifying properties based on histological analysis of the joints. (C) 2002 Published by Elsevier Science Ltd.
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