Synthesis and biological evaluation of amide derivatives of (5,6-dimethoxy-2,3-dihydro-1H-inden-1-yl)acetic acid as anti-inflammatory agents with reduced gastrointestinal ulcerogenecity
作者:Meenakshi Sharma、S.M. Ray
DOI:10.1016/j.ejmech.2007.08.008
日期:2008.10
A variety of amide derivatives of (5,6-dimethoxy-2,3-dihydro-1H-inden-1-yl)acetic acid were synthesized and screened for their analgesic and anti-inflammatory activities. The compounds were found to have longer activity profile exceeding that of indomethacin in carrageenan-induced rat paw edema model. Few selected compounds were also screened for their antipyretic, anti-arthritic and ulcerogenecity
合成了多种(5,6-二甲氧基-2,3-二氢-1H-茚满-1-基)乙酸的酰胺衍生物,并筛选了其镇痛和抗炎活性。在角叉菜胶诱导的大鼠爪水肿模型中,发现该化合物具有比消炎痛更长的活性谱。很少筛选出具有退烧,抗关节炎和致溃疡性的化合物。从这些研究可以得出结论,这些化合物尽管具有显着的解热活性,但并未通过抑制TNF-α发挥作用。在佐剂诱导的关节炎测定中,测试化合物未能阻止继发性炎症的发展。但是,这些化合物在100 mg / kg po的测试剂量水平下未显示溃疡形成