Palomba M, Pau A, Boatto G, Asproni B, Auzzas L, Cerri R, Arenare L, Filippelli W, Falcone G, Motola G
Dipartimento Farmaco Chimico Tossicologico, Facoltà di Farmacia, Università di Sassari, Italy.
Arch Pharm (Weinheim). 2000 Jan;333(1):17-26. doi: 10.1002/(sici)1521-4184(200001)333:1<17::aid-ardp17>3.0.co;2-0.
A series of substituted N-cycloalkyl benzamides, cinnamamides, and indole-3-carboxamides were synthesized and evaluated for their analgesic, antiinflammatory activities as well as for their gastrointestinal irritation liability. Indomethacin was used as reference drug in both tests. Compounds 1k, 1b, 1h, 1j, and 1g were the most active in the antiinflammatory paw edema inhibition test, with a sharply dose-dependent effect. In terms of the analgesic activity (acetic acid writhing test), the most active compound was 5a followed by 3a, but many other compounds were found to have a non-negligible potency. Even in this case, the effect was dose dependent.
合成了一系列取代的N-环烷基苯甲酰胺、肉桂酰胺和吲哚-3-甲酰胺,并对其镇痛、抗炎活性以及胃肠道刺激倾向进行了评估。在两项试验中均使用吲哚美辛作为参比药物。化合物1k、1b、1h、1j和1g在抗炎爪肿胀抑制试验中活性最高,具有明显的剂量依赖性效应。就镇痛活性(醋酸扭体试验)而言,活性最高的化合物是5a,其次是3a,但发现许多其他化合物也具有不可忽视的效力。即使在这种情况下,效应也是剂量依赖性的。