Lead compound optimization strategy (4) improving blood-brain barrier permeability through structural modification
文献类型：期刊论文
| 作者 | Hong Yu2; Zhou Yu1 ; Wang Jiang1; Liu Hong2
|
| 刊名 | Acta Pharmaceutica Sinica
 |
| 出版日期 | 2014 |
| 卷号 | 49期号:6页码:789-799 |
| 关键词 | blood-brain barrier structure optimization drug design central nervous system |
| ISSN号 | 0513-4870 |
| 其他题名 | 先导化合物结构优化策略(四)改善化合物的血脑屏障通透性 |
| 文献子类 | Article |
| 英文摘要 | Blood-brain barrier is a natural protection for human body. It protects central nervous system from the interruption and damage of xenobiotics. However, it prevents potential drugs aimed at central nervous system, thus becomes an obstruction for the development of central nervous system drugs. The recent development of blood-brain barrier permeability research and several lead optimization strategies to improve blood-brain barrier permeability are reviewed. These structure optimization methods include increasing lipophilicity, reducing hydrogen bond doners, simplifying molecule, increasing rigidity, lowering polar surface area, avoiding acid group, prodrug strategy, modifying into active transporter's substrates, as well as avoiding P-glycoprotein recognized structures. |
| 资助项目 | 国家杰出青年科学基金资助项目[00000000] |
| WOS研究方向 | Pharmacology & Pharmacy (provided by Clarivate Analytics) |
| 语种 | 中文 |
| CSCD记录号 | CSCD:5164107 |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/269336]  |
| 专题 | 药物化学研究室 药理学第一研究室 |
| 通讯作者 | Liu Hong |
| 作者单位 | 1.Key Laboratory of Receptor Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China. 2.School of Pharmacy, China Pharmaceutical University, Nanjing, Jiangsu 210009, China.; |
| 推荐引用方式 GB/T 7714 | Hong Yu,Zhou Yu,Wang Jiang,et al. Lead compound optimization strategy (4) improving blood-brain barrier permeability through structural modification[J]. Acta Pharmaceutica Sinica,2014,49(6):789-799. |
| APA | Hong Yu,Zhou Yu,Wang Jiang,&Liu Hong.(2014).Lead compound optimization strategy (4) improving blood-brain barrier permeability through structural modification.Acta Pharmaceutica Sinica,49(6),789-799. |
| MLA | Hong Yu,et al."Lead compound optimization strategy (4) improving blood-brain barrier permeability through structural modification".Acta Pharmaceutica Sinica 49.6(2014):789-799. |
入库方式： OAI收割
来源：上海药物研究所
浏览0
下载0
收藏0
其他版本
除非特别说明，本系统中所有内容都受版权保护，并保留所有权利。