Literature DB >> 23973169

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

Tao Zhou1, Robert C Hider, Peter Jenner, Bruce Campbell, Christopher J Hobbs, Sarah Rose, Mark Jairaj, Kayhan A Tayarani-Binazir, Alexander Syme.   

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 (4 g) was found to be the most active compound, with 106% AUC activity and 149% peak activity of L-dopa after oral administration.
Copyright © 2013 Elsevier Ltd. All rights reserved.

Entities:  

Keywords:  6-Hydroxydopamine (6-OHDA) lesioned rat; Parkinson’s disease; Prodrug; l-Dopa

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Year:  2013        PMID: 23973169     DOI: 10.1016/j.bmcl.2013.08.007

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  1 in total

1.  Enantiodivergent Steglich rearrangement of O-carboxylazlactones catalyzed by a chirality switchable helicene containing a 4-aminopyridine unit.

Authors:  Chien-Tien Chen; Cheng-Che Tsai; Pei-Kang Tsou; Gou-Tao Huang; Chin-Hui Yu
Journal:  Chem Sci       Date:  2016-08-25       Impact factor: 9.825

  1 in total

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