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Pyrroles and other heterocycles as inhibitors of p38 kinase.
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.
Affiliation
  • de Laszlo SE; Department of Medicinal Chemistry, Merck Research Laboratory, Rahway, NJ 07065, USA.
Bioorg Med Chem Lett ; 8(19): 2689-94, 1998 Oct 06.
Article in En | MEDLINE | ID: mdl-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.
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Database: MEDLINE Main subject: Pyrazoles / Pyrroles / Calcium-Calmodulin-Dependent Protein Kinases / Mitogen-Activated Protein Kinases / Enzyme Inhibitors / Furans Language: En Journal: Bioorg Med Chem Lett Year: 1998 Type: Article Affiliation country: United States
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PubMed Links

Database: MEDLINE Main subject: Pyrazoles / Pyrroles / Calcium-Calmodulin-Dependent Protein Kinases / Mitogen-Activated Protein Kinases / Enzyme Inhibitors / Furans Language: En Journal: Bioorg Med Chem Lett Year: 1998 Type: Article Affiliation country: United States