Synthesis and evaluation of NHC derivatives and 4′-fluorouridine prodrugs
文献类型：期刊论文
| 作者 | Xiang, Li3,4; Hu, Tianwen2,3; Xue, Haitao2,3; Pan, Wenfang2,3; Xie, Yuanchao1; Shen, Jingshan2,3,4
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| 刊名 | ORGANIC & BIOMOLECULAR CHEMISTRY
 |
| 出版日期 | 2023-03-29 |
| 卷号 | 21期号:13页码:2754-2767 |
| DOI | 10.1039/d3ob00268c |
| 文献子类 | Article |
| 英文摘要 | beta-d-N-4-Hydroxycytidine (NHC) derivatives with structural modifications at the C-4 & PRIME;, O-4 & PRIME; or C-6 position and 4 & PRIME;-fluorouridine prodrugs were synthesized and evaluated for their antiviral activities against respiratory syncytial virus (RSV) or influenza virus (IFV) in vitro. The NHC derivatives were found inactive, but 4 & PRIME;-fluorouridine and its prodrugs had potent anti-RSV and anti-IFV activities. 4 & PRIME;-Fluorouridine was proved to be a nucleoside with poor stability, but the tri-ester prodrugs exhibited enhanced stability, especially tri-isobutyrate ester 1a. This prodrug also showed excellent oral pharmacokinetic properties in rats, with potential to be an oral antiviral candidate. |
| WOS研究方向 | Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:000950316200001 |
| 出版者 | ROYAL SOC CHEMISTRY |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/309681]  |
| 专题 | 新药研究国家重点实验室 |
| 通讯作者 | Xie, Yuanchao; Shen, Jingshan |
| 作者单位 | 1.Lingang Lab, Shanghai 200031, Peoples R China 2.Univ Chinese Acad Sci, Beijing 100049, Peoples R China; 3.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai 201203, Peoples R China; 4.Nanjing Univ Chinese Med, Sch Chinese Mat Med, Nanjing 210023, Peoples R China; |
| 推荐引用方式 GB/T 7714 | Xiang, Li,Hu, Tianwen,Xue, Haitao,et al. Synthesis and evaluation of NHC derivatives and 4′-fluorouridine prodrugs[J]. ORGANIC & BIOMOLECULAR CHEMISTRY,2023,21(13):2754-2767. |
| APA | Xiang, Li,Hu, Tianwen,Xue, Haitao,Pan, Wenfang,Xie, Yuanchao,&Shen, Jingshan.(2023).Synthesis and evaluation of NHC derivatives and 4′-fluorouridine prodrugs.ORGANIC & BIOMOLECULAR CHEMISTRY,21(13),2754-2767. |
| MLA | Xiang, Li,et al."Synthesis and evaluation of NHC derivatives and 4′-fluorouridine prodrugs".ORGANIC & BIOMOLECULAR CHEMISTRY 21.13(2023):2754-2767. |
入库方式： OAI收割
来源：上海药物研究所
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