Abstract 5-Arylidene-2-oxo-4-thiazolidinones and 2-phenylimino analogues were evaluated for their antidegenerative activity on human chondrocyte cultures stimulated by IL-1 and for their inhibitory capability against matrix metalloproteinase-13. Our results indicated that 5-arylidene-4-thiazolidinone derivatives 1-9 exhibit antidegenerative activity and could block multiple cartilage destruction during the osteoarthritic process. Out of the selected compounds, (5-arylidene-2,4dioxothiazolidin-3-yl)acetic acids 7-9 showed significant effectiveness in reducing NO release and restoring normal levels of GAGs in chondrocytes treated with IL-1β. Moreover, benzoic acids 1, 5 and 6 proved to be effective MMP-13 inhibitors and were able to restore normal levels of GAGs.
|Titolo:||5-Arylidene-4-Thiazolidinone Derivatives Active as Antidegenerative Agents on Human Chondrocyte Cultures|
|Data di pubblicazione:||2013|
|Citazione:||5-Arylidene-4-Thiazolidinone Derivatives Active as Antidegenerative Agents on Human Chondrocyte Cultures / Panico A; Maccari R; Cardile V; Crascì L; Ronsisvalle S; Ottanà R.. - In: MEDICINAL CHEMISTRY. - ISSN 1573-4064. - 9:1(2013), pp. 1.84-1.90.|
|Appare nelle tipologie:||1.1 Articolo in rivista|