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

来自 : www.yxxb.com.cn:8081/aps/CN/ab 发布时间：2021-03-26

Abstract: Blood-brain barrier is a natural protection for human body.It protects central nervous systemfrom 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 increasinglipophilicity, 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.
2014年6月6日1. School of Pharmacy, China Pharmaceutical University, Nanjing 210009, China; 2. Key Laboratory of Receptor Research, Shanghai Institute of Materia Medica...血脑屏障; 结构优化; 药物设计; 中枢神经系统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