Synthesis and stability study of a modified phenylpropionic acid linker-based esterase-sensitive prodrug.
Synthesis and stability study of a modified phenylpropionic acid linker-based esterase-sensitive prodrug.
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基于修饰的苯丙酸连接基的酯酶敏感前药的合成和稳定性研究。
DOI：
10.1016/s0960-894x(02)00750-3
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发表时间：
2002
影响因子：
2.7
通讯作者：
Siahaan,TerunaJ
中科院分区：
文献类型：
--
作者：
Song,Xiaoping;Siahaan,TerunaJ
合成了一种具有酯酶敏感性的酰胺前药1。前药可以使用分离的猪酯酶和人血浆转化为药物。对氧磷是一种酯酶抑制剂，可抑制前药向药物的转化。前药1通过苯酚中间体9转化，然后进行内酯化反应，得到内酯2和药物。
An esterase-sensitive amide prodrug 1 with a modified phenylpropionic acid linker was synthesized. The prodrug can be converted to the drug using isolated porcine esterase and human plasma. Paraoxon, an esterase inhibitor, can inhibit prodrug-to-drug conversion. The conversion of prodrug 1 was via phenol intermediate 9 followed by a lactonization reaction to give lactone 2 and the drug.