Synthesis and antiinflammatory activity of trisubstituted pyrimidines and triazines
作者:Gregory B. Bennett、Robert B. Mason、Lee J. Alden、James B. Roach
DOI:10.1021/jm00205a006
日期:1978.7
A series of mono-, bi-, and tricyclic pyrimidines and as-triazines was prepared and their antiinflammatory activity measured against carrageenan-induced edema in the rat. The more active analogues (ED50), including 4-pyri-dylpyrimidines 4a (38), 4b (47), and 4g (49) and 2-hydroxypyrimidine 8r (43), were then tested against adjuvant-induced edema in the rat. None was active in the adjuvant arthritis
制备了一系列的单环,双环和三环嘧啶和三嗪,并测定了它们对角叉菜胶诱导的大鼠水肿的抗炎活性。然后测试了更具活性的类似物(ED50),包括4-pyri-dylpyrimidines 4a(38),4b(47)和4g(49)和2-hydroxypyrimidine 8r(43),以对抗佐剂诱导的大鼠水肿。在佐剂性关节炎模型中没有一个是活跃的。