Benzo[d]isothiazol-3-yl-benzamidines: a Class of Protective Agents on Culture of Human Cartilage and Chondrocytes Stimulated by IL-1β
✍ Scribed by Paola Vicini; Matteo Incerti; Venera Cardile; Floriana Garufi; Simone Ronsisvalle; Anna Maria Panico
- Book ID
- 102101042
- Publisher
- John Wiley and Sons
- Year
- 2007
- Tongue
- English
- Weight
- 115 KB
- Volume
- 2
- Category
- Article
- ISSN
- 1860-7179
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✦ Synopsis
Abstract
New derivatives of N‐benzo[d]isothiazol‐3‐yl‐benzamidine 6 a were synthesized as nonacidic anti‐inflammatory/antidegenerative agents. We investigated the influence of the amidines 6 a–j on the production of NO, PGE~2~, MMP‐3, COX‐2, ROS, and GAGs, key molecules involved in cartilage destruction in osteoarthritic diseases. The antidegenerative properties of the novel designed derivatives 6 b–j were improved with respect to N‐benzo[d]isothiazol‐3‐yl‐benzamidine 6 a. All of the compounds 6 a–j promoted the reduction of most of the IL‐1β‐induced harmful effects. Derivatives 6 d, 6 h, and 6 j were the most potent of all the tested compounds, particularly in the human chondrocyte culture model.