title: Aminothiazole derivatives with antidegenerative activity on cartilage.
abstract: 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.
authors.affiliation: Department of Pharmaceutical Sciences, Faculty of Pharmacy, University of Catania, V. le A. Doria 6, 95125 Catania, Italy.
authors.forename: Anna Maria
authors.initials: AM
authors.lastname: Panico
authors.forename: Athina
authors.initials: A
authors.lastname: Geronikaki
authors.forename: Remi
authors.initials: R
authors.lastname: Mgonzo
authors.forename: Venera
authors.initials: V
authors.lastname: Cardile
authors.forename: Barbara
authors.initials: B
authors.lastname: Gentile
authors.forename: Irini
authors.initials: I
authors.lastname: Doytchinova
mesh_terms: 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*
chemical_list: D000893:Anti-Inflammatory Agents; D006025:Glycosaminoglycans; D007375:Interleukin-1; D020011:Protective Agents; D013844:Thiazoles; D009569:Nitric Oxide