Synthesis and in vitro evaluation of 5-arylidene-3-hydroxyalkyl-2-phenylimino-4-thiazolidinones with antidegenerative activity on human chondrocyte cultures

Rosaria Ottanà, Rosanna Maccari, Rosella Ciurleo, Maria Gabriella Vigorita, Anna Maria Panico, Venera Cardile, Floriana Garufi, Simone Ronsisvalle

Research output: Contribution to journalArticle

43 Citations (Scopus)

Abstract

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-1β. 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 PGE2 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-1β.

Original languageEnglish
Pages (from-to)7618-7625
Number of pages8
JournalBioorganic and Medicinal Chemistry
Volume15
Issue number24
DOIs
Publication statusPublished - Dec 15 2007

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Chondrocytes
Interleukin-1
Human Activities
Matrix Metalloproteinases
Dinoprostone
Arthritis
Cell Survival
Theoretical Models
Cells
In Vitro Techniques

Keywords

  • 2-Phenylimino-4-thiazolidinones
  • Antidegenerative activity
  • Human chondrocyte
  • Osteoarthritis

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Biology
  • Organic Chemistry
  • Drug Discovery
  • Pharmaceutical Science

Cite this

Synthesis and in vitro evaluation of 5-arylidene-3-hydroxyalkyl-2-phenylimino-4-thiazolidinones with antidegenerative activity on human chondrocyte cultures. / Ottanà, Rosaria; Maccari, Rosanna; Ciurleo, Rosella; Vigorita, Maria Gabriella; Panico, Anna Maria; Cardile, Venera; Garufi, Floriana; Ronsisvalle, Simone.

In: Bioorganic and Medicinal Chemistry, Vol. 15, No. 24, 15.12.2007, p. 7618-7625.

Research output: Contribution to journalArticle

Ottanà, Rosaria ; Maccari, Rosanna ; Ciurleo, Rosella ; Vigorita, Maria Gabriella ; Panico, Anna Maria ; Cardile, Venera ; Garufi, Floriana ; Ronsisvalle, Simone. / Synthesis and in vitro evaluation of 5-arylidene-3-hydroxyalkyl-2-phenylimino-4-thiazolidinones with antidegenerative activity on human chondrocyte cultures. In: Bioorganic and Medicinal Chemistry. 2007 ; Vol. 15, No. 24. pp. 7618-7625.
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