Synthesis of cyclic prodrugs of Aggrastat and its analogue with a modified phenylpropionic acid linker.
Synthesis of cyclic prodrugs of Aggrastat and its analogue with a modified phenylpropionic acid linker.
复制标题
Aggrastat 及其类似物与修饰的苯丙酸连接体的环状前药的合成。
DOI：
10.1021/ol010282n
复制
发表时间：
2002
期刊：
影响因子：
5.2
通讯作者：
Siahaan,TerunaJ
中科院分区：
文献类型：
--
作者：
Song,Xiaoping;He,HenryT;Siahaan,TerunaJ
本工作的目的是分别从Aggrastat 2a及其类似物2b合成环状前药1a和1b，以提高其膜渗透性。如方案4所述，分别使用阿格司他或其类似物的-COOH基团与苯基丙酸接头3之间的酯键和哌啶基胺与接头3的-COOH基团之间的酰胺键形成环状前药1a和1b。
The objective of this work was to synthesize cyclic prodrugs1aand1bfrom Aggrastat2aand its analogue2b, respectively, to improve their membrane permeation. Cyclic prodrugs1aand1bwere formed using an ester bond between the -COOH group of Aggrastat or its analogue and the phenylpropionic acid linker3and an amide bond between the piperidinylamine and the -COOH group of the linker3, respectively, as outlined in Scheme 4.