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新型苯并呋喃类前药系列的设计、合成、对接及抗炎活性评价

Design, synthesis, docking and anti-inflammatory evaluation of novel series of benzofuran based prodrugs.

作者信息

Yadav Pratima, Singh Praveen, Tewari Ashish Kumar

机构信息

Department of Chemistry, Centre of Advance Studies, Faculty of Science, Banaras Hindu University, Varanasi 221 005, India.

Department of Chemistry, Centre of Advance Studies, Faculty of Science, Banaras Hindu University, Varanasi 221 005, India.

出版信息

Bioorg Med Chem Lett. 2014 May 15;24(10):2251-5. doi: 10.1016/j.bmcl.2014.03.087. Epub 2014 Apr 3.

Abstract

Several new benzofuran derivatives were synthesized, via appropriate synthetic route as anti-inflammatory agents. The anti-inflammatory activity of the prepared compounds was evaluated using carrageenan rat model. Among the synthesized compounds, some compounds showed comparable anti-inflammatory activity to nimesulide, the standard drug taken for anti-inflammatory studies. Docking study of the prepared compounds was performed for the study of interaction of molecules with the active site of COX-2. Preliminary biological studies and docking gave an interesting insight, into the validity of employing benzofuran analogues as good anti-inflammatory agent.

摘要

通过适当的合成路线合成了几种新的苯并呋喃衍生物作为抗炎剂。使用角叉菜胶大鼠模型评估所制备化合物的抗炎活性。在所合成的化合物中,一些化合物表现出与用于抗炎研究的标准药物尼美舒利相当的抗炎活性。对所制备的化合物进行对接研究,以研究分子与COX-2活性位点的相互作用。初步的生物学研究和对接为使用苯并呋喃类似物作为良好的抗炎剂的有效性提供了有趣的见解。

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