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Benzo[ d ]isothiazol‐3‐yl‐benzamidines: a Class of Protective Agents on Culture of Human Cartilage and Chondrocytes Stimulated by IL‐1β
Author(s) -
Vicini Paola,
Incerti Matteo,
Cardile Venera,
Garufi Floriana,
Ronsisvalle Simone,
Panico Anna Maria
Publication year - 2007
Publication title -
chemmedchem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.817
H-Index - 100
eISSN - 1860-7187
pISSN - 1860-7179
DOI - 10.1002/cmdc.200600157
Subject(s) - chemistry , chondrocyte , benzamidine , cartilage , stereochemistry , biochemistry , in vitro , enzyme , anatomy , biology
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.