| 9-(2-膦酰甲氧乙基)腺嘌呤及其位置异构体3-(2-膦酰甲氧乙基)腺嘌呤的合成和抗病毒活性研究 |
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| 引用本文： | 刘晓辉,王琳,贯宝各,孔漫,张兴权,陶佩珍,陈鸿珊.9-(2-膦酰甲氧乙基)腺嘌呤及其位置异构体3-(2-膦酰甲氧乙基)腺嘌呤的合成和抗病毒活性研究[J].药学学报,1996,31(2):112-117. |
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| 作者姓名： | 刘晓辉 王琳 贯宝各 孔漫 张兴权 陶佩珍 陈鸿珊 |
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| 作者单位： | 中国医学科学院、中国协和医科大学药物研究所，北京 100050; *中国医学科学院、中国协和医科大学医药生物技术研究所，北京 100050 |
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| 摘 要： |
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| 关 键 词： | 开链核苷酸 PMEA 位置异构体 抗病毒活性 |
| 收稿时间： | 1995-04-28 |
SYNTHESIS AND ANTI-VIRAL ACTIVITY OF 9-(2-PHOSPHONYL-METHOXYETHYL) ADENINE AND ITS REGIOISOMER 3-(2-PHOSPHONYLMETHOXYETHYL) ADENINE |
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| XH Liu,L Wang,BH Guan,M Kong,XQ Zhang,PZ Tao,HS Chen.SYNTHESIS AND ANTI-VIRAL ACTIVITY OF 9-(2-PHOSPHONYL-METHOXYETHYL) ADENINE AND ITS REGIOISOMER 3-(2-PHOSPHONYLMETHOXYETHYL) ADENINE[J].Acta Pharmaceutica Sinica,1996,31(2):112-117. |
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| Authors: | XH Liu L Wang BH Guan M Kong XQ Zhang PZ Tao HS Chen |
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| Abstract: | Phosphonylmethoxyethyl)adenine (1),PMEA,an acyclic nucleotide withbroad-spectrum antiviral activity was synthesized with some modifications of Holy's procedure.Simutaneously,an N-3 regioisomer(2)of PMEA and a by-preduct, formaldehyde di-2-(9-adenyl)ethyl] acetal(7)were seperated by silica gel chromatography in the ratio of 50:10:1.Compound(2)and(7) are new compounds that we have not yet found in literatures. The structure of them weredetermined with 1HNMR,2DNMR, MS and Spot test.Antiviral test showed that N-3 isomer(2)completely lost activity against both HIV-1 and HSV-1 in vitro. It seems that regiospecificity of theacyclic nucleotide structure is important for antiviral activity. |
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| Keywords: | PMEA Regioisomer Antiviral activity Acyclic nucleotide |
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