Design, synthesis and biological evaluation of L-dopa amide derivatives as potential prodrugs for the treatment of Parkinson's disease

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

doi:10.1016/j.ejmech.2010.05.062

Design, synthesis and biological evaluation of L-dopa amide derivatives as potential prodrugs for the treatment of Parkinson's disease

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

King's College London

Research output: Contribution to journal › Article › peer-review

24 Citations (Scopus)

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. (C) 2010 Elsevier Masson SAS. All rights reserved.

Original language	English
Pages (from-to)	4035 - 4042
Number of pages	8
Journal	EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume	45
Issue number	9
DOIs	https://doi.org/10.1016/j.ejmech.2010.05.062
Publication status	Published - Sept 2010

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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 - 4042. https://doi.org/10.1016/j.ejmech.2010.05.062

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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. (C) 2010 Elsevier Masson SAS. All rights reserved.",

author = "Tao Zhou and Hider, {Robert C.} and Peter Jenner and Bruce Campbell and Hobbs, {Christopher J.} and Sarah Rose and Mark Jairaj and Tayarani-Binazir, {Kayhan A.} and Alexander Syme",

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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

PY - 2010/9

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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. (C) 2010 Elsevier Masson SAS. All rights reserved.

AB - 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. (C) 2010 Elsevier Masson SAS. All rights reserved.

U2 - 10.1016/j.ejmech.2010.05.062

DO - 10.1016/j.ejmech.2010.05.062

M3 - Article

VL - 45

SP - 4035

EP - 4042

JO - EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

JF - EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

IS - 9

ER -

Design, synthesis and biological evaluation of L-dopa amide derivatives as potential prodrugs for the treatment of Parkinson's disease

Abstract

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