Hori N, Tsukamoto G, Imamura A, Ohashi M, Saito T, Yoshino K
New Drug Research Laboratories, Kanebo, Ltd., Osaka, Japan.
Chem Pharm Bull (Tokyo). 1992 Sep;40(9):2387-90. doi: 10.1248/cpb.40.2387.
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.
合成了一系列2-(4-甲基苯基)苯并噻唑，并使用佐剂诱导的关节炎大鼠模型进行评估。通过血凝试验发现了这类影响免疫反应的目标化合物。4-乙酰氧基-2-(4-甲基苯基)苯并噻唑(7m)，即KB-2683，在佐剂诱导的关节炎大鼠模型中活性最强，并被选作进一步评估。与非甾体抗炎药不同，化合物7m没有抗炎或镇痛活性。然而，它在增强的迟发型超敏反应中显示出免疫调节活性。
