Preparation and stability studies on dipeptide mimetic α-methyldopa prodrugs

H. P. Wang*, J. R. Ma, J. S. Lee, W. L. Luo

*Corresponding author for this work

Research output: Contribution to journalJournal Article peer-review

2 Scopus citations

Abstract

Amino acids D-phenylglycine and D-p-hydroxyphenylglycine were attached onto α-methyldopa to form prodrugs 1a, 1b and 1c. As dipeptides in nature, these prodrugs were expected to be absorbed in small intestine via dipeptide-mediated carrier transport systems. Preliminary studies revealed that the prodrugs were stable in pH 7.4 phosphate buffer solutions (t( 1/2 ) > 10 h).These compounds demonstrated satisfactory stability toward enzymatic degradation in a mucosa preparation isolated from rat intestine, indicating that they might be feasible to be formulated as oral prodrugs of α-methyldopa.

Original languageEnglish
Pages (from-to)47-58
Number of pages12
JournalChinese Pharmaceutical Journal
Volume47
Issue number1
StatePublished - 1995
Externally publishedYes

Keywords

  • D-phenylglycine and D-p-hydroxyphenylglycine
  • dipeptide mimetic α-methyldopa prodrugs
  • dipeptide-mediated carrier transport systems
  • synthesis and stability

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