A series of benzobisthiazoles were screened for antiinflammatory activity in the carrageenan paw edema and adjuvant arthritis tests. Compound 26, 2,6-bis(N,N-diethylamino)benzo[1,2-d:5,4-d']bisthiazole, was found to inhibit the swelling of the uninjected paw in the prophylactic adjuvant arthritis model with an ED50 of 2.3 mg/kg orally. As with most compounds of this series, 26 was inactive in acute
筛选了一系列苯并双
噻唑类在角叉菜胶足肿胀和辅助性关节炎试验中的抗炎活性。在预防性佐剂关节炎模型中,发现化合物26,2,6-双(N,N-二乙
氨基)苯并[1,2-d:5,4-d']双
噻唑可抑制未注射的爪肿胀。口服ED50为2.3 mg / kg。与该系列的大多数化合物一样,在急性炎症模型(如爪
水肿)中,有26种没有活性。像类
固醇一样,它在肉芽肿袋试验中显示出活性,但没有抑制环氧合酶,表明其作用方式不同于经典的非甾体类抗炎药(N
SAID's)。在高于产生抗炎活性的剂量时,26具有一定的免疫调节特性。