Journal
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 45, Issue 9, Pages 4035-4042Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2010.05.062
Keywords
L-dopa; Dopamide; Parkinson's disease; Prodrug; 6-hydroxydopamine (6-OHDA) lesioned rat
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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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