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Pyrroles and other heterocycles as inhibitors of p38 kinase.

Bioorganic & medicinal chemistry letters (1999-01-05)
S E de Laszlo, D Visco, L Agarwal, L Chang, J Chin, G Croft, A Forsyth, D Fletcher, B Frantz, C Hacker, W Hanlon, C Harper, M Kostura, B Li, S Luell, M MacCoss, N Mantlo, E A O'Neill, C Orevillo, M Pang, J Parsons, A Rolando, Y Sahly, K Sidler, S J O'Keefe
ABSTRACT

Investigation of furans, pyrroles and pyrazolones identified 3-pyridyl-2,5-diaryl-pyrroles as potent, orally bioavailable inhibitors of p38 kinase. 3-(4-pyridyl-2-(4-fluoro-phenyl)-5-(4-methylsulfinylphenyl)-pyrrol e (L-167307) reduces secondary paw swelling in the rat adjuvant arthritis model: ID50 = 7.4 mg/kg/b.i.d.