Provided are carboxylic ester derivatives of formula (I), methods of preparing them, and methods for using them. These compounds are prodrugs of D-isoglutamyl-[D/L]-tryptophan. The in vitro bioconversion of some of the prodrugs to the parent drug D-isoglutamyl-D-tryptophan (or thymodepressin) was tested in human hepatocytes and in human blood. In vivo pharmacokinetic studies following oral administration of some of the prodrugs to rats are also reported.
提供了公式(I)的
羧酸酯衍
生物,其制备方法以及使用方法。这些化合物是D-异谷
氨酰-[D/L]-色
氨酸的前药。对一些前药在人类肝细胞和人类血液中转化为母药D-异谷
氨酰-
D-色氨酸(或胸腺抑制素)的体外
生物转化进行了测试。还报告了将一些前药口服给大鼠后的体内药代动力学研究。