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一些新型2-亚芳基-4-(联苯-4-基)-丁-3-烯-4-内酯的合成、反应及其生物活性研究

Syntheses and reactions of some new 2-arylidene-4-(biphenyl-4-yl)-but-3-en-4-olides with a study of their biological activity.

作者信息

Khan M S Y, Husain A

机构信息

Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Jamia Hamdard (Hamdard University), New Delhi, India.

出版信息

Pharmazie. 2002 Jul;57(7):448-52.

Abstract

2-Arylidene-4-(biphenyl-4-yl)but-3-en-4-olides also known as 3-arylidene-5-(biphenyl-4-yl)-2(3H)-furanones were prepared from 3-(4-phenyl-benzoyl) propionic acid and aromatic aldehydes. Some of the selected butenolides were reacted with ammonia and benzylamine to give corresponding pyrrolones and N-benzylpyrrolones respectively, which were characterized on the basis of 1H NMR and MS data and elemental analysis results. These compounds were tested for anti-inflammatory and anti-microbial actions. A few compounds were found to have promising anti-inflammatory activity while a fair in number of compounds showed a good anti-fungal activity and a promising antibacterial activity against S. aureus and E. coli.

摘要

2-亚芳基-4-(联苯-4-基)丁-3-烯-4-内酯,也被称为3-亚芳基-5-(联苯-4-基)-2(3H)-呋喃酮,由3-(4-苯基-苯甲酰基)丙酸和芳香醛制备而成。一些选定的丁烯内酯分别与氨和苄胺反应,得到相应的吡咯酮和N-苄基吡咯酮,通过1H NMR、MS数据以及元素分析结果对其进行表征。对这些化合物进行了抗炎和抗菌活性测试。发现少数化合物具有良好的抗炎活性,相当数量的化合物表现出良好的抗真菌活性以及对金黄色葡萄球菌和大肠杆菌有一定的抗菌活性。

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