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Pyrroles and other heterocycles as inhibitors of p38 kinase
S E de Laszlo1, D Visco, L Agarwal
1Department of Medicinal Chemistry, Merck Research Laboratory, Rahway, NJ 07065, USA.
Bioorganic & Medicinal Chemistry Letters
|January 5, 1999
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.