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具有抗炎和镇痛活性的新型咪唑基乙酸衍生物的合成。

Synthesis of new imidazolyl acetic acid derivatives with anti-inflammatory and analgesic activities.

作者信息

Khalifa Maha M, Abdelbaky Nayira A

机构信息

Pharmaceutical Chemistry, Al-Azhar University (Girls), Cairo, Egypt.

出版信息

Arch Pharm Res. 2008 Apr;31(4):419-23. doi: 10.1007/s12272-001-1173-x. Epub 2008 May 1.

Abstract

We synthesized 2-(4-(4-fluorobenzylidene)-2-(4-fluorophenyl) 5-oxo-4,5-dihydroimidazol-1-yl) acetic acid 3. Chlorination afforded the chloro derivative 4, which reacted with different amines and hydrazine to afford compounds 5-8. Pyrazole, pyrazolone, and thiazolidinone derivatives were also synthesized from Imidazol-1-ylacetic acid hydrazide 8 to give compounds 9-12. Compounds were then evaluated for their anti-inflammatory activity against carrageenan-induced rat paw edema and their analgesic activity using the writhing test in albino mice. Compounds 5, 9, 10, 12 exhibited maximum anti-inflammatory activity, and all the compounds inhibited writhing, with 10 and 12 being two times more effective than the reference standard.

摘要

我们合成了2-(4-(4-氟亚苄基)-2-(4-氟苯基)-5-氧代-4,5-二氢咪唑-1-基)乙酸3。氯化反应得到氯代衍生物4,其与不同的胺和肼反应得到化合物5-8。吡唑、吡唑啉酮和噻唑烷酮衍生物也由咪唑-1-基乙酰肼8合成得到化合物9-12。然后使用角叉菜胶诱导的大鼠足爪水肿模型评估化合物的抗炎活性,并使用白化小鼠扭体试验评估其镇痛活性。化合物5、9、10、12表现出最大的抗炎活性,并且所有化合物均抑制扭体反应,其中10和12的效果比参考标准高两倍。

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