Novel disease-modifying antirheumatic drugs. I. Synthesis and antiarthritic activity of 2-(4-methylphenyl)benzothiazoles.

Chem Pharm Bull (Tokyo)

New Drug Research Laboratories, Kanebo, Ltd., Osaka, Japan.

Published: September 1992

A series of 2-(4-methylphenyl)benzothiazoles was synthesized and evaluated using an adjuvant-induced arthritic rat model. This class of desired compounds affecting the immune response was found using hemagglutination assay. 4-Acetoxy-2-(4-methylphenyl)benzothiazole (7m), KB-2683, was most potent in the adjuvant-induced arthritic rat model and selected for further evaluation. In contrast to nonsteroidal antiinflammatory drugs, compound 7m showed no antiinflammatory or analgesic activities. It did, however, show an immunomodulatory activity in enhanced delayed type hypersensitivity.

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http://dx.doi.org/10.1248/cpb.40.2387DOI Listing

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