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Design, synthesis and biological evaluation of peptide derivatives of L-dopa as anti-parkinsonian agents.
Bioorg Med Chem Lett. 2013 Oct 01; 23(19):5279-82.BM

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.

Authors+Show Affiliations

School of Food Science and Biotechnology, Zhejiang Gongshang University, Hangzhou, Zhejiang 310035, PR China. taozhou@zjgsu.edu.cnNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article

Language

eng

PubMed ID

23973169

Citation

Zhou, Tao, et al. "Design, Synthesis and Biological Evaluation of Peptide Derivatives of L-dopa as Anti-parkinsonian Agents." Bioorganic & Medicinal Chemistry Letters, vol. 23, no. 19, 2013, pp. 5279-82.
Zhou T, Hider RC, Jenner P, et al. Design, synthesis and biological evaluation of peptide derivatives of L-dopa as anti-parkinsonian agents. Bioorg Med Chem Lett. 2013;23(19):5279-82.
Zhou, T., Hider, R. C., Jenner, P., Campbell, B., Hobbs, C. J., Rose, S., Jairaj, M., Tayarani-Binazir, K. A., & Syme, A. (2013). Design, synthesis and biological evaluation of peptide derivatives of L-dopa as anti-parkinsonian agents. Bioorganic & Medicinal Chemistry Letters, 23(19), 5279-82. https://doi.org/10.1016/j.bmcl.2013.08.007
Zhou T, et al. Design, Synthesis and Biological Evaluation of Peptide Derivatives of L-dopa as Anti-parkinsonian Agents. Bioorg Med Chem Lett. 2013 Oct 1;23(19):5279-82. PubMed PMID: 23973169.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Design, synthesis and biological evaluation of peptide derivatives of L-dopa as anti-parkinsonian agents. AU - Zhou,Tao, AU - Hider,Robert C, AU - Jenner,Peter, AU - Campbell,Bruce, AU - Hobbs,Christopher J, AU - Rose,Sarah, AU - Jairaj,Mark, AU - Tayarani-Binazir,Kayhan A, AU - Syme,Alexander, Y1 - 2013/08/11/ PY - 2013/06/14/received PY - 2013/07/15/revised PY - 2013/08/02/accepted PY - 2013/8/27/entrez PY - 2013/8/27/pubmed PY - 2014/4/8/medline KW - 6-Hydroxydopamine (6-OHDA) lesioned rat KW - Parkinson’s disease KW - Prodrug KW - l-Dopa SP - 5279 EP - 82 JF - Bioorganic & medicinal chemistry letters JO - Bioorg Med Chem Lett VL - 23 IS - 19 N2 - 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. SN - 1464-3405 UR - https://www.unboundmedicine.com/medline/citation/23973169/Design_synthesis_and_biological_evaluation_of_peptide_derivatives_of_L_dopa_as_anti_parkinsonian_agents_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0960-894X(13)00936-0 DB - PRIME DP - Unbound Medicine ER -