The development of novel inhibitors of tumor necrosis factor-alpha production based on substituted [5,5]-bicyclic pyrozolones
Novel substituted [5,5]-bicyclic pyrzazolones are presented as inhibitors of tumor necrosis factor-{alpha} (TNF-{alpha}) production. Many of these compounds show low nanomolar activity against lipopolysaccaride (LPS)-induced TNF-{alpha} production in THP-1 cells. This class of molecules was co-cryst...
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Published in: | Bioorganic & medicinal chemistry Vol. 14; no. (16) ; 2004 |
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Main Authors: | , , , , , , , , , , , , , , , , |
Format: | Journal Article |
Language: | English |
Published: |
United States
16-11-2010
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Subjects: | |
Online Access: | Get full text |
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Summary: | Novel substituted [5,5]-bicyclic pyrzazolones are presented as inhibitors of tumor necrosis factor-{alpha} (TNF-{alpha}) production. Many of these compounds show low nanomolar activity against lipopolysaccaride (LPS)-induced TNF-{alpha} production in THP-1 cells. This class of molecules was co-crystallized with mutated p38, and several analogs showed good oral bioavailability in the rat. Oral activity of these compounds in the rat iodoacetate model for osteoarthritis is discussed. |
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Bibliography: | USDOE |
ISSN: | 0968-0896 1464-3391 |