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Design, synthesis and biological evaluation of L-dopa amide derivatives as potential prodrugs for the treatment of Parkinson's disease

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
Pages (from-to)4035 - 4042
Number of pages8
JournalEUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume45
Issue number9
DOIs
Publication statusPublished - Sep 2010

King's Authors

Abstract

A range of amide derivatives of L-dopa were synthesized and investigated for their pharmacological activity and their ability to be converted to L-dopa using the unilaterally 6-hydroxydopamine (6-OHDA)-lesioned rat, as an experimental model of Parkinson's disease. The diacetyl derivative of L-dopa amide (11b) was found to be more active than L-dopa after its oral administration and generated plasma levels of L-dopa in the therapeutic range for an antiparkinsonian effect in man. (C) 2010 Elsevier Masson SAS. All rights reserved.

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