Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 23, Issue 19, Pages 5279-5282Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2013.08.007
Keywords
L-Dopa; Prodrug; Parkinson's disease; 6-Hydroxydopamine (6-OHDA) lesioned rat
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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. (C) 2013 Elsevier Ltd. All rights reserved.
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