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Design, synthesis and biological evaluation of peptide derivatives of L-dopa as anti-parkinsonian agents

Research output: Contribution to journalArticle

Tao Zhou, Robert C. Hider, Peter Jenner, Bruce Campbell, Christopher J. Hobbs, Sarah Rose, Mark Jairaj, Kayhan A. Tayarani-Binazir, Alexander Syme

Original languageEnglish
Article numberN/A
Pages (from-to)5279-5282
Number of pages4
JournalBIOORGANIC AND MEDICINAL CHEMISTRY LETTERS
Volume23
Issue number19
DOIs
Publication statusPublished - 1 Oct 2013

King's Authors

Abstract

A series of dipeptide derivatives of L-dopa were synthesized and investigated for their pharmacological activity using the unilaterally 6-hydroxydopamine (6-OHDA)-lesioned rat as an experimental model of Parkinson's disease. Among them, (S)-isopropyl 2-(2-amino-2-methylpropanamido)-3-(3,4-dihydroxyphenyl) propanoate (4g) was found to be the most active compound, with 106% AUC activity and 149% peak activity of L-dopa after oral administration.

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