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非甾体抗炎药。VII. 5-甲基-10,11-二氢-5H-吡咯并[1,2-b][1,2,5]苯并三氮杂䓬-11-乙酸及其10-芳酰基衍生物的合成与抗炎活性

Non-steroidal antiinflammatory agents. VII. Synthesis and antiinflammatory activity of 5-methyl-10,11-dihydro-5H-pyrrolo [1,2-b] [1,2,5]benzotriazepine-11-acetic acid and its 10-aroyl derivatives.

作者信息

Stefancich G, Artico M, Silvestri R, Prosini P P, Pantaleoni G, Giorgi R, Palumbo G

机构信息

Dipartimento di Studi Farmaceutici, Università La Sapienza, Roma.

出版信息

Farmaco. 1990 Jul;45(7-8):817-31.

PMID:2282117
Abstract

The synthesis of 5-methyl-10,11-dihydro-5H-pyrrolo [1,2-b] [1,2,5]benzotriazepine-11-acetic acid and its 10-aroyl derivatives is reported. Compounds were evaluated for antiinflammatory activity by the carrageenin-induced rat paw edema method. Antinociceptic activity was tested by the hot plate and Randall-Selitto tests. General neuropsychopharmacological effects were also screened. All test compounds showed antiinflammatory effect comparable to that of tolmetin.

摘要

报道了5-甲基-10,11-二氢-5H-吡咯并[1,2 - b][1,2,5]苯并三氮杂卓-11-乙酸及其10-芳酰基衍生物的合成。通过角叉菜胶诱导的大鼠足爪水肿法评估化合物的抗炎活性。通过热板法和兰德尔-塞利托试验测试镇痛活性。还筛选了一般神经精神药理学作用。所有测试化合物均显示出与托美汀相当的抗炎作用。

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