Anti-inflammatory and analgesic amides: New developments

被引:0
|
作者
Palomba, M
Pau, A
Boatto, G
Asproni, B
Auzzas, L
Cerri, R
Arenare, L
Filippelli, W
Falcone, G
Motola, G
机构
[1] Univ Sassari, Dipartimento Farmaco Chim Tossicol, I-07100 Sassari, Italy
[2] Dipartimento Chim Farmaceut & Tossicol, I-80131 Naples, Italy
[3] Univ Naples 2, Fac Med & Chirurg, Ist Farmacol & Tossicol, I-80138 Naples, Italy
关键词
analgesic and antiinflammatory agents; substituted N-cycloalkyl benzamides; cinnamamides; and indole-3-carboxamides;
D O I
10.1002/(SICI)1521-4184(200001)333:1<17::AID-ARDP17>3.0.CO;2-0
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
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.
引用
收藏
页码:17 / 26
页数:10
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