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Optimisation of the Anti-Trypanosoma brucei Activity of the Opioid Agonist U50488

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Optimisation of the Anti-Trypanosoma brucei Activity of the Opioid Agonist U50488. / Smith, Victoria C.; Cleghorn, Laura A. T.; Woodland, Andrew; Spinks, Daniel; Hallyburton, Irene; Collie, Iain T.; Mok, N. Yi; Norval, Suzanne; Brenk, Ruth; Fairlamb, Alan H.; Frearson, Julie A.; Read, Kevin D.; Gilbert, Ian H.; Wyatt, Paul G.

In: ChemMedChem, Vol. 6, No. 10, 04.10.2011, p. 1832-1840.

Research output: Contribution to journalArticle

Harvard

Smith, VC, Cleghorn, LAT, Woodland, A, Spinks, D, Hallyburton, I, Collie, IT, Mok, NY, Norval, S, Brenk, R, Fairlamb, AH, Frearson, JA, Read, KD, Gilbert, IH & Wyatt, PG 2011, 'Optimisation of the Anti-Trypanosoma brucei Activity of the Opioid Agonist U50488' ChemMedChem, vol 6, no. 10, pp. 1832-1840.

APA

Smith, V. C., Cleghorn, L. A. T., Woodland, A., Spinks, D., Hallyburton, I., Collie, I. T., Mok, N. Y., Norval, S., Brenk, R., Fairlamb, A. H., Frearson, J. A., Read, K. D., Gilbert, I. H., & Wyatt, P. G. (2011). Optimisation of the Anti-Trypanosoma brucei Activity of the Opioid Agonist U50488. ChemMedChem, 6(10), 1832-1840doi: 10.1002/cmdc.201100278

Vancouver

Smith VC, Cleghorn LAT, Woodland A, Spinks D, Hallyburton I, Collie IT et al. Optimisation of the Anti-Trypanosoma brucei Activity of the Opioid Agonist U50488. ChemMedChem. 2011 Oct 4;6(10):1832-1840.

Author

Smith, Victoria C.; Cleghorn, Laura A. T.; Woodland, Andrew; Spinks, Daniel; Hallyburton, Irene; Collie, Iain T.; Mok, N. Yi; Norval, Suzanne; Brenk, Ruth; Fairlamb, Alan H.; Frearson, Julie A.; Read, Kevin D.; Gilbert, Ian H.; Wyatt, Paul G. / Optimisation of the Anti-Trypanosoma brucei Activity of the Opioid Agonist U50488.

In: ChemMedChem, Vol. 6, No. 10, 04.10.2011, p. 1832-1840.

Research output: Contribution to journalArticle

Bibtex - Download

@article{c2816fe3b662461f9b6f45ba67f41bb4,
title = "Optimisation of the Anti-Trypanosoma brucei Activity of the Opioid Agonist U50488",
author = "Smith, {Victoria C.} and Cleghorn, {Laura A. T.} and Andrew Woodland and Daniel Spinks and Irene Hallyburton and Collie, {Iain T.} and Mok, {N. Yi} and Suzanne Norval and Ruth Brenk and Fairlamb, {Alan H.} and Frearson, {Julie A.} and Read, {Kevin D.} and Gilbert, {Ian H.} and Wyatt, {Paul G.}",
year = "2011",
volume = "6",
number = "10",
pages = "1832--1840",
journal = "ChemMedChem",
issn = "1860-7179",

}

RIS (suitable for import to EndNote) - Download

TY - JOUR

T1 - Optimisation of the Anti-Trypanosoma brucei Activity of the Opioid Agonist U50488

A1 - Smith,Victoria C.

A1 - Cleghorn,Laura A. T.

A1 - Woodland,Andrew

A1 - Spinks,Daniel

A1 - Hallyburton,Irene

A1 - Collie,Iain T.

A1 - Mok,N. Yi

A1 - Norval,Suzanne

A1 - Brenk,Ruth

A1 - Fairlamb,Alan H.

A1 - Frearson,Julie A.

A1 - Read,Kevin D.

A1 - Gilbert,Ian H.

A1 - Wyatt,Paul G.

AU - Smith,Victoria C.

AU - Cleghorn,Laura A. T.

AU - Woodland,Andrew

AU - Spinks,Daniel

AU - Hallyburton,Irene

AU - Collie,Iain T.

AU - Mok,N. Yi

AU - Norval,Suzanne

AU - Brenk,Ruth

AU - Fairlamb,Alan H.

AU - Frearson,Julie A.

AU - Read,Kevin D.

AU - Gilbert,Ian H.

AU - Wyatt,Paul G.

PY - 2011/10/4

Y1 - 2011/10/4

N2 - <p>Screening of the Sigma-Aldrich Library of Pharmacologically Active Compounds (LOPAC) against cultured Trypanosoma brucei, the causative agent of African sleeping sickness, resulted in the identification of a number of compounds with selective antiproliferative activity over mammalian cells. These included (+)-(1R,2R)-U50488, a weak opioid agonist with an EC50 value of 59 nm as determined in our T. brucei in vitro assay reported previously. This paper describes the modification of key structural elements of U50488 to investigate structure-activity relationships (SAR) and to optimise the antiproliferative activity and pharmacokinetic properties of this compound.</p>

AB - <p>Screening of the Sigma-Aldrich Library of Pharmacologically Active Compounds (LOPAC) against cultured Trypanosoma brucei, the causative agent of African sleeping sickness, resulted in the identification of a number of compounds with selective antiproliferative activity over mammalian cells. These included (+)-(1R,2R)-U50488, a weak opioid agonist with an EC50 value of 59 nm as determined in our T. brucei in vitro assay reported previously. This paper describes the modification of key structural elements of U50488 to investigate structure-activity relationships (SAR) and to optimise the antiproliferative activity and pharmacokinetic properties of this compound.</p>

KW - antiprotozoal agents

KW - human African trypanosomiasis

KW - medicinal chemistry

KW - U50488

KW - HUMAN AFRICAN TRYPANOSOMIASIS

KW - DERIVATIVES

KW - DISEASES

UR - http://ukpmc.ac.uk/articles/PMC3229842

U2 - 10.1002/cmdc.201100278

DO - 10.1002/cmdc.201100278

M1 - Article

JO - ChemMedChem

JF - ChemMedChem

SN - 1860-7179

IS - 10

VL - 6

SP - 1832

EP - 1840

ER -

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