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杂环吲哚衍生物的合成与抗炎活性

Synthesis and antiinflammatory activity of heterocyclic indole derivatives.

作者信息

Rani Preeti, Srivastava V K, Kumar Ashok

机构信息

Department of Pharmacology, LLRM Medical College, Meerut, U.P.-250004, India.

出版信息

Eur J Med Chem. 2004 May;39(5):449-52. doi: 10.1016/j.ejmech.2003.11.002.

Abstract

Chalcones of indole 1-5 and their corresponding products; pyrazolines 6-10 and azo compounds 11-15 were synthesised and evaluated for their antiinflammatory activity against carrageenan induced oedema in albino rats at a dose of 50 mg x kg(-1) oral. The structure of compounds was confirmed by IR, (1)H-NMR and mass spectral data. All the compounds of this series showed promising antiinflammatory activity. The most active compound of this series is 3-[1-acetyl-5-(p-hydroxyphenyl)-2-pyrazolin-3-yl]indole (7) was found to be most potent, which has shown higher percent of inhibition of oedema, lower ulcerogenic liability and acute toxicity than the standard drug phenylbutazone.

摘要

合成了吲哚1 - 5的查耳酮及其相应产物;吡唑啉6 - 10和偶氮化合物11 - 15,并以50 mg x kg(-1)口服剂量对白化病大鼠角叉菜胶诱导的水肿进行抗炎活性评估。通过红外光谱、(1)H - NMR和质谱数据确认了化合物的结构。该系列所有化合物均显示出有前景的抗炎活性。该系列中最具活性的化合物3 - [1 - 乙酰基 - 5 - (对羟基苯基)-2 - 吡唑啉 - 3 - 基]吲哚(7)被发现是最有效的,其显示出比标准药物保泰松更高的水肿抑制百分比、更低的致溃疡倾向和急性毒性。

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