Title of article
The development of monocyclic pyrazolone based cytokine synthesis inhibitors
Author/Authors
Adam Golebiowski، نويسنده , , Jennifer A. Townes، نويسنده , , Matthew J. Laufersweiler، نويسنده , , Todd A. Brugel، نويسنده , , Michael P. Clark، نويسنده , , Cynthia M. Clark، نويسنده , , Jane F. Djung، نويسنده , , Steven K. Laughlin، نويسنده , , Mark P. Sabat، نويسنده , , Roger G. Bookland، نويسنده , , John C. VanRens، نويسنده , , Biswanath De، نويسنده , , Lily C. Hsieh، نويسنده , , Michael J. Janusz، نويسنده , , Richard L. Walter and Alan M. Friedman، نويسنده , , Mark E. Webster، نويسنده , , Marlene J. Mekel، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2005
Pages
5
From page
2285
To page
2289
Abstract
4-Aryl-5-pyrimidyl based cytokine synthesis inhibitors that contain a novel monocyclic, pyrazolone heterocyclic core are described. Many of these inhibitors showed low nanomolar activity against LPS-induced TNF-α production. One of the compounds (6e) was found to be efficacious in the rat iodoacetate (RIA) in vivo model of osteoarthritis. The X-ray crystal structure of a pyrazolone inhibitor cocrystallized with mutated p38 (mp38) is presented.
Keywords
Cytokine synthesis inhibitors , p38 kinase
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2005
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
795574
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