PHENYTOIN-LIPID CONJUGATES AS POTENTIAL PRODRUGS OF PHENYTOIN

被引：21

作者：

SCRIBA, GKE

机构：

[1] Department of Pharmaceutical Chemistry, University of Münster, Münster, D-48149

来源：

ARCHIV DER PHARMAZIE | 1993年 / 326卷 / 08期

关键词：

D O I：

10.1002/ardp.19933260810

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Phenytoin-1-triglycerides and phenytoin-2-triglycerides were synthesized as potential prodrugs of phenytoin by covalent binding of 3-hydroxymethylphenytoin by succinic acid to the positions 1 and 2 of diglycerides, respectively. The corresponding 1- and 2-monoglycerides were prepared. In addition, replacement of glycerol by 3-hydroxy-2-hydroxymethylpropionic acid furnished lipids that allowed direct coupling of 3-hydroxymethylphenytoin. The lipid conjugates proved to be substrates for pancreatic lipase in vitro.

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页码：477 / 481

页数：5

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