Aminothiazole derivatives with antidegenerative activity on cartilage.
A series of 2-dialkylamino-N-(4-substituted thiazolyl-2)acetamides and 3-dialkylamino-N-(4-substituted thiazolyl-2)propionamides were synthesized and evaluated for their anti-inflammatory activity. Encouraging results led us to investigate the effect of these compounds on NO production and GAGs release. Their effects were evaluated in vitro on the metabolism of pig cartilage, treated with IL-1beta. The amount of glycosaminoglycans (GAGs) and the production of nitric oxide (NO) in the culture medium were determined. The results, obtained, showed that all compounds, in the presence of IL-1beta, blocked the cartilage breakdown, with different behavior. A quantitative structure-activity relationship (QSAR) study was performed.
Panico
Anna Maria
AM
Department of Pharmaceutical Sciences, Faculty of Pharmacy, University of Catania, V. le A. Doria 6, 95125 Catania, Italy.
Geronikaki
Athina
A
Mgonzo
Remi
R
Cardile
Venera
V
Gentile
Barbara
B
Doytchinova
Irini
I
D000818:Animals; D000893:Anti-Inflammatory Agents / Q000737:chemistry / Q000494:pharmacology; D002356:Cartilage / Q000187:drug effects* / Q000378:metabolism; D002357:Cartilage Diseases / Q000188:drug therapy; D046508:Culture Techniques; D004305:Dose-Response Relationship, Drug; D006025:Glycosaminoglycans / Q000378:metabolism; D007375:Interleukin-1; D009569:Nitric Oxide / Q000378:metabolism; D020011:Protective Agents / Q000737:chemistry* / Q000494:pharmacology; D021281:Quantitative Structure-Activity Relationship; D013552:Swine; D013844:Thiazoles / Q000737:chemistry* / Q000494:pharmacology*
D000893:Anti-Inflammatory Agents; D006025:Glycosaminoglycans; D007375:Interleukin-1; D020011:Protective Agents; D013844:Thiazoles; D009569:Nitric Oxide