Pyrroles and other heterocycles as inhibitors of p38 kinase.
作者信息
de Laszlo S E, Visco D, Agarwal L, Chang L, Chin J, Croft G, Forsyth A, Fletcher D, Frantz B, Hacker C, Hanlon W, Harper C, Kostura M, Li B, Luell S, MacCoss M, Mantlo N, O'Neill E A, Orevillo C, Pang M, Parsons J, Rolando A, Sahly Y, Sidler K, O'Keefe S J
机构信息
Department of Medicinal Chemistry, Merck Research Laboratory, Rahway, NJ 07065, USA.
出版信息
Bioorg Med Chem Lett. 1998 Oct 6;8(19):2689-94. doi: 10.1016/s0960-894x(98)00495-8.
PMID:9873604
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.
摘要
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