Toja E, Selva D, Schiatti P
J Med Chem. 1984 May;27(5):610-6. doi: 10.1021/jm00371a010.
Novel 3-alkyl-2-aryl-3H- naphth [1,2-d]imidazoles were synthesized and evaluated as antiinflammatory agents in the carrageenin-induced paw edema, cotton pellet induced granuloma, and adjuvant-induced polyarthritis assays in rats. The analgesic, antipyretic, and gastroulcerogenic effects were also tested. Structure-activity relationships are discussed. One of the compounds, 3-(1-methylethyl)-2-(4-methoxyphenyl)-3H- naphth [1,2-d]imidazole (35), was selected for clinical trials as a nonacidic antiinflammatory and analgesic agent.
合成了新型3-烷基-2-芳基-3H-萘并[1,2-d]咪唑,并在角叉菜胶诱导的大鼠足爪水肿、棉球诱导的肉芽肿和佐剂诱导的多关节炎试验中作为抗炎剂进行了评价。还测试了其镇痛、解热和致胃溃疡作用。讨论了构效关系。其中一种化合物3-(1-甲基乙基)-2-(4-甲氧基苯基)-3H-萘并[1,2-d]咪唑(35)被选为作为非酸性抗炎和镇痛药进行临床试验。