Synthesis and in vitro evaluation of 5-arylidene-3-hydroxyalkyl-2-phenylimino-4-thiazolidinones with antidegenerative activity on human chondrocyte cultures.
5-Arylidene-3-hydroxyalkyl-2-phenylimino-4-thiazolidinones (7,8) were synthesized and evaluated for their antidegenerative activity on human chondrocyte cultures stimulated by IL-1beta. This in vitro model has proven to be a useful experimental model to reproduce the mechanisms involved in arthritic diseases. The cell viability, the amount of GAGs, the production of NO and PGE(2) and the inhibition of MMP-3 were measured. Several thiazolidinones 7 and 8 exhibited the ability to block the production or action of the degenerative factors induced by IL-1beta.
Ottanà
Rosaria
R
Dipartimento Farmaco-chimico, Università di Messina, Polo Universitario dell'Annunziata, 98168 Messina, Italy.
Maccari
Rosanna
R
Ciurleo
Rosella
R
Vigorita
Maria Gabriella
MG
Panico
Anna Maria
AM
Cardile
Venera
V
Garufi
Floriana
F
Ronsisvalle
Simone
S
D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000138:chemical synthesis* / Q000494:pharmacology*; D001168:Arthritis / Q000188:drug therapy; D002470:Cell Survival / Q000187:drug effects; D002478:Cells, Cultured; D019902:Chondrocytes / Q000187:drug effects* / Q000276:immunology; D004353:Drug Evaluation, Preclinical; D006801:Humans; D007097:Imines / Q000138:chemical synthesis* / Q000494:pharmacology; D007213:Indomethacin / Q000494:pharmacology; D053583:Interleukin-1beta / Q000494:pharmacology; D008954:Models, Biological; D012015:Reference Standards; D053778:Thiazolidines / Q000138:chemical synthesis* / Q000494:pharmacology*
D000894:Anti-Inflammatory Agents, Non-Steroidal; D007097:Imines; D053583:Interleukin-1beta; D053778:Thiazolidines; D007213:Indomethacin