| Aldisin及其衍生物的合成和α-葡萄糖苷酶抑制活性研究 |
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| 引用本文： | 曾向潮,徐石海,李毅群,王渝芳.Aldisin及其衍生物的合成和α-葡萄糖苷酶抑制活性研究[J].有机化学,2005,25(8):954-958. |
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| 作者姓名： | 曾向潮 徐石海 李毅群 王渝芳 |
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| 作者单位： | 1. 暨南大学化学系,广州,510632
2. 中山大学化学与化学工程学院,广州,510275 |
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| 基金项目： | 国家高技术研究发展计划(863计划)，广东省科技厅科技计划 |
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| 摘 要： | 以三氯氧磷为环化试剂, 回流状态下, N-(2-吡咯甲酰基)-β-丙氨酸经分子内酰化环化反应, 合成了吡咯2,3-c]氮杂二酮稠环化合物Aldisin及其衍生物1-Methylaldisin和3-Bromoaldisin, 通过1H NMR, 13C NMR, IR, FABMS和元素分析对其结构进行了表征. 以X射线衍射法研究了3-Methylaldisin的晶体结构. 测定了三个化合物对α-葡萄糖苷酶的抑制作用.
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| 关 键 词： | Aldisin 1-Methylaldisin 环化反应 晶体结构 α-葡萄糖苷酶 |
| 收稿时间： | 2004-7-1 |
| 修稿时间： | 2004年7月1日 |
Syntheses and α-Glucosidase Inhibitions of Aldisin and Its Derivatives |
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| ZENG,Xiang-Chao,XU,Shi-Hai,LI,Yi-Qun,WANG,Yu-Fang.Syntheses and α-Glucosidase Inhibitions of Aldisin and Its Derivatives[J].Chinese Journal of Organic Chemistry,2005,25(8):954-958. |
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| Authors: | ZENG Xiang-Chao XU Shi-Hai LI Yi-Qun WANG Yu-Fang |
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| Institution: | (Department of Chemistry, Jinan University, Guangzhou 510632)(School of Chemistry and Chemical Engineering, Sun Yat-sen University, Guangzhou 510275) |
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| Abstract: | Aldisin (6,7-dihydropyrrolo2,3-c]azepine-4,8(1H,5H)-dione) and its derivatives, 1-methy-laldisin and 3-bromoaldisin, were synthesized by cyclization of 3-(pyrrole-2-carbonyl)amino] propionic acids in phosphorus oxychloride under reflux. Their structures were characterized by 1H NMR, 13C NMR, FABMS, IR spectra and elemental analy-sis. The crystal structure of 1-methylaldisin was determined by single-crystal X-ray diffraction. And the α-glucosidase inhibitions of these compounds have also been studied. |
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| Keywords: | Aldisin 1-Methylaldisin |
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