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新型吡唑和二氢吡唑衍生物的合成及其作为潜在抗炎和镇痛药的研究。

Synthesis of novel pyrazole and dihydropyrazoles derivatives as potential anti-inflammatory and analgesic agents.

机构信息

Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Cairo University, Egypt.

出版信息

Arch Pharm Res. 2012 May;35(5):807-21. doi: 10.1007/s12272-012-0507-y. Epub 2012 May 29.

Abstract

Novel dihydropyrazole 5-8, 10 and pyrazole derivatives 12, 14, 15, 17 were synthesized. The structures of the newly synthesized compounds were elucidated by spectral and elemental analyses. The anti-inflammatory activity of all new compounds was evaluated using the carrageenan-induced rat paw edema test using indomethacin and celecoxib as reference drugs. The most active derivatives as anti-inflammatory agents were accordingly tested for their analgesic activity using the p-benzoquinone-induced writhing method in mice and results revealed that these compounds had also good analgesic activity. The ulcerogenic liability of the selected compounds was also evaluated. Results showed that the selected derivatives had anti-inflammatory activity comparable to or slightly lower than the reference drugs, reaching about 82% inhibition with a considerable gastric safety profile.

摘要

新型二氢吡唑 5-8、10 和吡唑衍生物 12、14、15、17 被合成出来。新合成化合物的结构通过光谱和元素分析得到阐明。所有新化合物的抗炎活性均通过角叉菜胶诱导的大鼠足肿胀试验进行评估,使用吲哚美辛和塞来昔布作为参考药物。抗炎活性最高的衍生物被进一步用于通过小鼠对苯醌诱导的扭体法评估其镇痛活性,结果表明这些化合物也具有良好的镇痛活性。所选化合物的致溃疡倾向也得到了评估。结果表明,所选衍生物具有与参考药物相当或略低的抗炎活性,达到约 82%的抑制率,并且具有相当好的胃安全性。

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