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

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Design, synthesis and biological evaluation of peptide derivatives of L-dopa as anti-parkinsonian agents. / Zhou, Tao; Hider, Robert C.; Jenner, Peter; Campbell, Bruce; Hobbs, Christopher J.; Rose, Sarah; Jairaj, Mark; Tayarani-Binazir, Kayhan A.; Syme, Alexander.

In: BIOORGANIC AND MEDICINAL CHEMISTRY LETTERS, Vol. 23, No. 19, N/A, 01.10.2013, p. 5279-5282.

Research output: Contribution to journalArticle

Harvard

Zhou, T, Hider, RC, Jenner, P, Campbell, B, Hobbs, CJ, Rose, S, Jairaj, M, Tayarani-Binazir, KA & Syme, A 2013, 'Design, synthesis and biological evaluation of peptide derivatives of L-dopa as anti-parkinsonian agents', BIOORGANIC AND MEDICINAL CHEMISTRY LETTERS, vol. 23, no. 19, N/A, pp. 5279-5282. https://doi.org/10.1016/j.bmcl.2013.08.007

APA

Zhou, T., Hider, R. C., Jenner, P., Campbell, B., Hobbs, C. J., Rose, S., ... Syme, A. (2013). Design, synthesis and biological evaluation of peptide derivatives of L-dopa as anti-parkinsonian agents. BIOORGANIC AND MEDICINAL CHEMISTRY LETTERS, 23(19), 5279-5282. [N/A]. https://doi.org/10.1016/j.bmcl.2013.08.007

Vancouver

Zhou T, Hider RC, Jenner P, Campbell B, Hobbs CJ, Rose S et al. Design, synthesis and biological evaluation of peptide derivatives of L-dopa as anti-parkinsonian agents. BIOORGANIC AND MEDICINAL CHEMISTRY LETTERS. 2013 Oct 1;23(19):5279-5282. N/A. https://doi.org/10.1016/j.bmcl.2013.08.007

Author

Zhou, Tao ; Hider, Robert C. ; Jenner, Peter ; Campbell, Bruce ; Hobbs, Christopher J. ; Rose, Sarah ; Jairaj, Mark ; Tayarani-Binazir, Kayhan A. ; Syme, Alexander. / Design, synthesis and biological evaluation of peptide derivatives of L-dopa as anti-parkinsonian agents. In: BIOORGANIC AND MEDICINAL CHEMISTRY LETTERS. 2013 ; Vol. 23, No. 19. pp. 5279-5282.

Bibtex Download

@article{9c258cadd5ff4b61828870ea53551c2a,
title = "Design, synthesis and biological evaluation of peptide derivatives of L-dopa as anti-parkinsonian agents",
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 = "L-Dopa, Prodrug, Parkinson's disease, 6-Hydroxydopamine (6-OHDA) lesioned rat, PRODRUGS, DISEASE, SOLUBILITY, STABILITY, DELIVERY",
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",
year = "2013",
month = "10",
day = "1",
doi = "10.1016/j.bmcl.2013.08.007",
language = "English",
volume = "23",
pages = "5279--5282",
journal = "Bioorganic & medicinal chemistry letters",
issn = "0960-894X",
publisher = "Elsevier Limited",
number = "19",

}

RIS (suitable for import to EndNote) Download

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

PY - 2013/10/1

Y1 - 2013/10/1

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 (4g) was found to be the most active compound, with 106% AUC activity and 149% peak activity of L-dopa after oral administration.

AB - 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.

KW - L-Dopa

KW - Prodrug

KW - Parkinson's disease

KW - 6-Hydroxydopamine (6-OHDA) lesioned rat

KW - PRODRUGS

KW - DISEASE

KW - SOLUBILITY

KW - STABILITY

KW - DELIVERY

U2 - 10.1016/j.bmcl.2013.08.007

DO - 10.1016/j.bmcl.2013.08.007

M3 - Article

VL - 23

SP - 5279

EP - 5282

JO - Bioorganic & medicinal chemistry letters

JF - Bioorganic & medicinal chemistry letters

SN - 0960-894X

IS - 19

M1 - N/A

ER -

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