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3. Aminothiazole derivatives with antidegenerative activity on cartilage.

Author

Panico AM, Geronikaki A, Mgonzo R, Cardile V, Gentile B, and Doytchinova I

Subjects
Animals, Anti-Inflammatory Agents chemistry, Anti-Inflammatory Agents pharmacology, Cartilage metabolism, Cartilage Diseases drug therapy, Culture Techniques, Dose-Response Relationship, Drug, Glycosaminoglycans metabolism, Interleukin-1, Nitric Oxide metabolism, Protective Agents pharmacology, Swine, Cartilage drug effects, Protective Agents chemistry, Quantitative Structure-Activity Relationship, Thiazoles chemistry, Thiazoles pharmacology
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.

Published
2003
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4. Synthesis and antiinflammatory activity of some new thiazole derivatives.

Author

Mgonzo R, Geronikaki A, and Kourounakis PN

Subjects
Animals, Anti-Inflammatory Agents, Non-Steroidal pharmacology, Carrageenan, Chromatography, Thin Layer, Edema chemically induced, Edema prevention & control, Indomethacin pharmacology, Mice, Mice, Inbred AKR, Thiazoles pharmacology, Anti-Inflammatory Agents, Non-Steroidal chemical synthesis, Thiazoles chemical synthesis
Published
1995

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