Khanum Shaukath A, Shashikanth Sheena, Deepak A V
Department of Studies in Chemistry, University of Mysore, Manasagangotri, Mysore 570 006, India.
Bioorg Chem. 2004 Aug;32(4):211-22. doi: 10.1016/j.bioorg.2004.04.003.
A series of substituted benzophenone analogues has been synthesized and evaluated as orally active anti-inflammatory agents with reduced side effects. The anti-inflammatory and ulcerogenic activities of the compounds were compared with naproxen, indomethacin, and phenylbutazone. In carrageenan-induced foot pad edema assay, benzophenone analogues showed an interesting anti-inflammatory activity. In the air-pouch test, some of the analogues reduced the total number of leukocytes of the exudate, which indicates inhibition of prostaglandin production. Side effects of the compounds were examined on gastric mucosa, in the liver and stomach. None of the compounds showed significant side effects compared with nonsteroidal anti-inflammatory drugs such as indomethacin and naproxen.
已合成了一系列取代二苯甲酮类似物,并将其作为具有降低副作用的口服活性抗炎剂进行了评估。将这些化合物的抗炎和致溃疡活性与萘普生、吲哚美辛和保泰松进行了比较。在角叉菜胶诱导的足垫水肿试验中,二苯甲酮类似物显示出有趣的抗炎活性。在气袋试验中,一些类似物减少了渗出液中白细胞的总数,这表明对前列腺素生成有抑制作用。在胃黏膜、肝脏和胃部对这些化合物的副作用进行了检查。与吲哚美辛和萘普生等非甾体抗炎药相比,这些化合物均未显示出明显的副作用。