Novel disease-modifying antirheumatic drugs. I. Synthesis and antiarthritic activity of 2-(4-methylphenyl)benzothiazoles.
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.
Hori
N
N
New Drug Research Laboratories, Kanebo, Ltd., Osaka, Japan.
Tsukamoto
G
G
Imamura
A
A
Ohashi
M
M
Saito
T
T
Yoshino
K
K
D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000138:chemical synthesis* / Q000494:pharmacology; D001169:Arthritis, Experimental / Q000188:drug therapy*; D006384:Hemagglutination / Q000187:drug effects; D006968:Hypersensitivity, Delayed / Q000188:drug therapy; D008297:Male; D051379:Mice; D008807:Mice, Inbred BALB C; D051381:Rats; D011916:Rats, Inbred F344; D013844:Thiazoles / Q000138:chemical synthesis* / Q000494:pharmacology
D000894:Anti-Inflammatory Agents, Non-Steroidal; D013844:Thiazoles