| 1H-吡咯-2(5H)-酮类化合物的合成及生物活性 |
| 投稿时间：2012-05-11 修订日期：2012-06-20 点此下载全文 |
| 引用本文：赵方振,庄春林,郭子照,盛春泉,姚建忠,缪震元,张万年.1H-吡咯-2(5H)-酮类化合物的合成及生物活性[J].药学实践杂志,2012,30(6):430~432,456 |
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| 基金项目:上海市科委生物医药重点项目资助(09431901700). |
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| 中文摘要:目的 研究5位连有取代苯基的1H-吡咯-2(5H)-酮类化合物生物活性。方法 在吡咯酮的5位引入各种取代苯基,合成出目标化合物,所有化合物1H NMR和MS等谱确证;通过荧光偏振法测定化合物对蛋白的抑制常数Ki。结果 所有13个目标化合物都能抑制蛋白的结合,其中化合物4e的Ki达到阳性对照药的5倍。结论 5位苯环的取代基团对活性影响很大,吸电子基团取代活性高于亲电子基团,其中硝基取代活性最强。 |
| 中文关键词:1H-吡咯-2(5H)-酮 化学合成 生物活性 |
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| Synthesis and biological activity of 1H-pyrrol-2(5H)-ones |
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| Abstract:Objective To study the biological activity of 1H-pyrrol-2(5H)-ones which introduced substituted phenyl group as side chain. Methods By introduction of 5-substituted phenyl group, a serial 1H-pyrrol-2(5H)-ones were synthesized and their structures were confirmed by 1H NMR and MS. The binding constant Ki was assayed by the fluorescence polarization binding assay method. Results Thirteen title compounds exhibited stronger protein binding activities and compound 4e showed five times higher than positive drug.Conclusion The introduction of electron-attracting groups was beneficial to improve their activities. Among them, the nitro group was preferred group. |
| keywords:1H-pyrrol-2(5H)-one chemical synthesis biological activity |
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