Design, synthesis and anti-HBV activity of L-amino acid ester prodrugs of acyclic nucleoside phosphonates
文献类型：期刊论文
| 作者 | FU Xiaozhong2; JIANG Saihong1; YANG Yushe1 ; JI Ruyun1
|
| 刊名 | Acta Pharmaceutica Sinica
 |
| 出版日期 | 2008 |
| 卷号 | 43期号:5页码:495-503 |
| 关键词 | acyclic nucleoside phosphonate L-amino acid prodrug |
| ISSN号 | 0513-4870 |
| 其他题名 | 新型非环核苷膦酸L-氨基酸酯类化合物的设计、合成与抗乙型肝炎病毒活性 |
| 文献子类 | Article |
| 英文摘要 | To design and synthesis a series of novel L-amino acid esters prodrugs of acyclic nucleoside phosphonates with more potent anti-HBV activity, adefovir dipivoxil was used as lead compound, according to the results of enhanced oral bioavailability and antiviral activities of nucleoside L-amino acid ester prodrugs. Eleven novel L-amino acid ester prodrugs of acyclic nucleoside phosphonates were designed and synthesized, their anti-HBV activities were evaluated in HepG2 2.2.15 cells. Eight compounds exhibited antiviral activity, and compound 11 showed the most potent anti-HBV activity and highest selective index in vitro （EC_(50) 0. 095 2 mumol · L~(-1), SI 69523）. Moreover, by analyzing the primary structure and activity relationship of these compounds, it could be suggested that L-amino acid ester strategy has significant potential in the acyclic nucleoside phosphonates prodrug design. |
| WOS研究方向 | Pharmacology & Pharmacy (provided by Clarivate Analytics) |
| 语种 | 中文 |
| CSCD记录号 | CSCD:3295572 |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/268091]  |
| 专题 | 药物化学研究室 |
| 作者单位 | 1.State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Shanghai Institute for Biological Sciences, Chinese Academy of Science, Shanghai 201203, China. 2.School of Pharmacy, Guiyang Medical College, Guiyang, Guizhou 550004, China.; |
| 推荐引用方式 GB/T 7714 | FU Xiaozhong,JIANG Saihong,YANG Yushe,et al. Design, synthesis and anti-HBV activity of L-amino acid ester prodrugs of acyclic nucleoside phosphonates[J]. Acta Pharmaceutica Sinica,2008,43(5):495-503. |
| APA | FU Xiaozhong,JIANG Saihong,YANG Yushe,&JI Ruyun.(2008).Design, synthesis and anti-HBV activity of L-amino acid ester prodrugs of acyclic nucleoside phosphonates.Acta Pharmaceutica Sinica,43(5),495-503. |
| MLA | FU Xiaozhong,et al."Design, synthesis and anti-HBV activity of L-amino acid ester prodrugs of acyclic nucleoside phosphonates".Acta Pharmaceutica Sinica 43.5(2008):495-503. |
入库方式： OAI收割
来源：上海药物研究所
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