Synthesis and activity of hydroxyethylene peptidomimetic inhibitors of humanβ-secretase  

羟亚乙基拟肽类人β-分泌酶抑制剂的合成和活性(英文)

作　　者：马超[1] 王月华[2] 杨晓鸣[1] 邹晓民[1] 吕杨[1] 杜冠华[2] 徐萍[1] 

机构地区：[1]北京大学药学院药物化学系,北京100191 [2]中国医学科学院药物研究所,北京100050

出　　处：《Journal of Chinese Pharmaceutical Sciences》2008年第3期215-220,共6页中国药学（英文版）

基　　金：National Natural Science Foundation of China(Grant No.30772650 and 20772008).

摘　　要：A series of β-secretase peptidomimetic inhibitors with Leu＊Ala hydroxyethylene dipeptide isostere were synthesized and their β-secretase inhibitory activities were measured. The most potent compound N9 showed an inhibitory rate of 59.66% （10 mg/mL）. Compound N9 might be further modified by means of computational chemical methodology.本文设计并合成了一系列含Leu*Ala羟亚乙基二肽电子等排体的β-分泌酶拟肽类抑制剂,并测定了β-分泌酶抑制活性。活性最强的化合物N9显示59.66%(10 mg/mL)抑制率。化合物N9可经计算化学方法进一步优化。

关 键 词：β-Secretase inhibitors Hydroxyethylene isostere SYNTHESIS Bioactivity 

分 类 号：R914[医药卫生—药物化学] R96[医药卫生—药学]