| 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,贯宝和,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(2). |
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| 作者姓名： | 刘晓辉 王琳 贯宝和 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，中国医学科学院中国协和医科大学医药生物技术研究所 |
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| 基金项目： | 卫生部抗艾滋病药物研究（八五攻关课题） |
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| 摘 要： | 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刘晓辉，王琳，贯宝和，孔漫，张兴权，陶佩珍，陈鸿珊（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...
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| 关 键 词： | 开链核苷酸 PMEA 位置异构体 抗病毒活性 |
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(2). |
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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: | Acyclic nucleotide PMEA Regioisomer Antiviral activity |
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