Paris G Y, Garmaise D L, Cimon D G, Swett L, Carter G W, Young P
J Med Chem. 1980 Jan;23(1):9-13. doi: 10.1021/jm00175a003.
Mono-, bis-, and tris[1-(p-chlorobenzoyl)-5-methoxy-2-methylindole-3-acetyl]glycerides and 1,3-dialkanoyl-2-[1-(p-chlorobenzoyl)-5-methoxy-2-methylindole-3-acetyl]glycerides were synthesized and evaluated for antiinflammatory activity in the rat paw carrageenin edema assay. Three of the most active compounds (4, 18a, and 18e) were tested in the rat adjuvant arthritis model and found to be essentially equivalent in activity to indomethacin. On a molar basis, the acute gastric irritating properties of 18a and 18e were seven to eight times less than indomethacin, resulting in a 2.5- to 3-fold improvement in the ratio of antiedema activity to ulcerogenicity.
合成了单[1-(对氯苯甲酰基)-5-甲氧基-2-甲基吲哚-3-乙酰基]甘油酯、双[1-(对氯苯甲酰基)-5-甲氧基-2-甲基吲哚-3-乙酰基]甘油酯和三[1-(对氯苯甲酰基)-5-甲氧基-2-甲基吲哚-3-乙酰基]甘油酯以及1,3-二烷酰基-2-[1-(对氯苯甲酰基)-5-甲氧基-2-甲基吲哚-3-乙酰基]甘油酯，并在大鼠足爪角叉菜胶水肿试验中评估了它们的抗炎活性。对三种活性最高的化合物（4、18a和18e）在大鼠佐剂性关节炎模型中进行了测试，发现其活性与吲哚美辛基本相当。以摩尔计，18a和18e的急性胃刺激性比吲哚美辛小7至8倍，抗水肿活性与致溃疡性之比提高了2.5至3倍。
