Synthesis of novel ADPR analogues: substitution of pyrophosphate linkage by dipeptide  

具有二肽结构的ADPR类似物的合成(英文)

作　　者：张超[1] 杨振军[1] 张亮仁[1] 张礼和[1] 

机构地区：[1]北京大学药学院天然药物及仿生药物国家重点实验室,北京100083

出　　处：《Journal of Chinese Pharmaceutical Sciences》2007年第4期262-267,共6页中国药学（英文版）

基　　金：National Natural Science Foundation of China(Grant No.20472007);the Research Found for the DocroralProgram of Higher Education

摘　　要：For investigating the biological function of ADPR, four novel analogues （compounds 2-5） in which the pyrophosphate linkage was replaced by the aspartic acid dipeptide were synthesized. 5＇-Amino adenosine or its analogues was used as the starting material, liquid phase peptide synthesis strategy was used to construct these ADPR analogues. The structures were characterized by 1H NMR and HRMS spectra. This study provides a versatile synthesis of peptide modified ADPR analogues and helps to understand the structure-activity relationship of ADPR.为进一步探讨ADPR的生物学功能,本文设计并合成了用天门冬氨酸二肽代替焦磷酸结构的一类新型ADPR类似物。通过以5'-氨基腺苷或其模拟物为起始原料,采用类似于液相肽的合成方法,成功地构建了四个目标分子,其结构经1HNMR、HRMS等进行了鉴定。本研究为新型ADPR类似物的合成提供了一条便利途径。

关 键 词：ADPR NUCLEOSIDE ANALOGUES Synthesis 

分 类 号：R914[医药卫生—药物化学]