5-Arylidene-4-Thiazolidinone Derivatives Active as Antidegenerative Agents on Human Chondrocyte Cultures

Title:5-Arylidene-4-Thiazolidinone Derivatives Active as Antidegenerative Agents on Human Chondrocyte Cultures

Volume: 9 Issue: 1

Author(s): Annamaria Panico, Rosanna Maccari, Venera Cardile, Lucia Crascì, Simone Ronsisvalle and Rosaria Ottanà

Affiliation:

Keywords: Antidegenerative activity, Anti-inflammatory activity, 5-Arylidene-2-phenylimino-4-thiazolidinones, 5-Arylidene- 4-thiazolidinones, Glycosaminoglycans, Human chondrocytes, Matrix metalloproteinase-13, Nitric oxide

Abstract: 5-Arylidene-2-oxo-4-thiazolidinones and 2-phenylimino analogues were evaluated for their antidegenerative activity on human chondrocyte cultures stimulated by IL-1β 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- 2,4-dioxothiazolidin-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.

Cite this article as:

Panico Annamaria, Maccari Rosanna, Cardile Venera, Crascì Lucia, Ronsisvalle Simone and Ottanà Rosaria, 5-Arylidene-4-Thiazolidinone Derivatives Active as Antidegenerative Agents on Human Chondrocyte Cultures, Medicinal Chemistry 2013; 9 (1) . https://dx.doi.org/10.2174/1573406411309010084