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Design, synthesis and biological evaluation of L-dopa amide derivatives as potential prodrugs for the treatment of Parkinson's disease.
Eur J Med Chem. 2010 Sep; 45(9):4035-42.EJ

Abstract

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.

Authors+Show Affiliations

School of Food Science and Biotechnology, Zhejiang Gongshang University, Hangzhou, Zhejiang, 310035, PR China.No 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

20646792

Citation

Zhou, Tao, et al. "Design, Synthesis and Biological Evaluation of L-dopa Amide Derivatives as Potential Prodrugs for the Treatment of Parkinson's Disease." European Journal of Medicinal Chemistry, vol. 45, no. 9, 2010, pp. 4035-42.
Zhou T, Hider RC, Jenner P, et al. Design, synthesis and biological evaluation of L-dopa amide derivatives as potential prodrugs for the treatment of Parkinson's disease. Eur J Med Chem. 2010;45(9):4035-42.
Zhou, T., Hider, R. C., Jenner, P., Campbell, B., Hobbs, C. J., Rose, S., Jairaj, M., Tayarani-Binazir, K. A., & Syme, A. (2010). Design, synthesis and biological evaluation of L-dopa amide derivatives as potential prodrugs for the treatment of Parkinson's disease. European Journal of Medicinal Chemistry, 45(9), 4035-42. https://doi.org/10.1016/j.ejmech.2010.05.062
Zhou T, et al. Design, Synthesis and Biological Evaluation of L-dopa Amide Derivatives as Potential Prodrugs for the Treatment of Parkinson's Disease. Eur J Med Chem. 2010;45(9):4035-42. PubMed PMID: 20646792.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Design, synthesis and biological evaluation of L-dopa amide derivatives as potential prodrugs for the treatment of Parkinson's disease. 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 - 2010/06/02/ PY - 2010/03/26/received PY - 2010/05/25/revised PY - 2010/05/26/accepted PY - 2010/7/22/entrez PY - 2010/7/22/pubmed PY - 2010/12/14/medline SP - 4035 EP - 42 JF - European journal of medicinal chemistry JO - Eur J Med Chem VL - 45 IS - 9 N2 - 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. SN - 1768-3254 UR - https://www.unboundmedicine.com/medline/citation/20646792/Design_synthesis_and_biological_evaluation_of_L_dopa_amide_derivatives_as_potential_prodrugs_for_the_treatment_of_Parkinson's_disease_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0223-5234(10)00433-2 DB - PRIME DP - Unbound Medicine ER -