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Design,synthesis and biological evaluation of peptide derivatives of l-dopa as anti-parkinsonian agents |
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| Authors: | Tao Zhou Robert C. Hider Peter Jenner Bruce Campbell Christopher J. Hobbs Sarah Rose Mark Jairaj Kayhan A. Tayarani-Binazir Alexander Syme |
| Affiliation: | 1. School of Food Science and Biotechnology, Zhejiang Gongshang University, Hangzhou, Zhejiang 310035, PR China;2. Division of Pharmaceutical Science, King’s College London, Franklin-Wilkins Building, 150 Stamford Street, London SE1 9NH, UK;3. NDRC, School of Biomedical and Health Sciences, King’s College, London SE1 1UL, UK;4. Proximagen Neuroscience plc, Hodgkin Building, King’s College, London SE1 1UL, UK |
| 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. |
| Keywords: | Prodrug Parkinson’s disease 6-Hydroxydopamine (6-OHDA) lesioned rat |
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