Synthesis of novel pyrazole and dihydropyrazoles derivatives as potential anti-inflammatory and analgesic agents
Synthesis of novel pyrazole and dihydropyrazoles derivatives as potential anti-inflammatory and analgesic agents
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DOI：
10.1007/s12272-012-0507-y
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发表时间：
2012-05-01
影响因子：
6.7
通讯作者：
Abdelsalam, Rania M.
中科院分区：
文献类型：
--
作者：
Abd-El Gawad, Nagwa M.;Georgey, Hanan H.;Abdelsalam, Rania M.
合成了新型二氢吡唑5-8、10及其衍生物12、14、15、17。新合成的化合物的结构经波谱和元素分析确证。以消炎痛和塞来昔布为参比药物，采用角叉菜胶致大鼠足肿胀实验评价新化合物的抗炎活性。采用对苯二酚致小鼠扭体法对最具抗炎活性的化合物进行了镇痛活性测试，结果表明这些化合物也具有良好的镇痛活性。还对所选化合物的致溃性进行了评估。结果表明，所选择的衍生物具有与参比药物相当或略低于参比药物的抗炎活性，抑制率约为82%，具有相当的胃部安全性。
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.