5-di-tert-butyl-4-hydroxybenzylidene)pyrrolidin-2-ones was synthesized and evaluated as candidate antiinflammatory/analgesic agents as well as dual inhibitors of prostaglandin and leukotriene synthesis. Some compounds that showed dual inhibitory activity were found to possess equipotent antiinflammatory activities to indomethacin, with reduced ulcerogenic effects. One of the compounds, N-methoxy-3-(3,5-d
合成了一系列3-(3,5-二叔丁基-
4-羟基亚苄基)
吡咯烷酮-2-酮,并作为候选抗炎/止痛药以及
前列腺素和
白三烯合成的双重
抑制剂进行了评估。发现某些具有双重抑制活性的化合物具有与
消炎痛同等的抗炎活性,并具有降低的致溃疡作用。发现其中一种化合物N-甲氧基-3-(3,5-二叔丁基-
4-羟基苄叉基)
吡咯烷-2--2-烯比
吲哚美辛或
吡罗昔康具有更宽的安全系数,因此被选择用于详细评估为临床应用的候选药物。