Dissemin is shutting down on January 1st, 2025

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Wiley, ChemMedChem, 10(6), p. 1832-1840, 2011

DOI: 10.1002/cmdc.201100278

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

Journal article published in 2011 by Victoria C. Smith, Laura A. T. Cleghorn ORCID, Andrew Woodland, Daniel Spinks, Irene Hallyburton, Iain T. Collie, N. Yi Mok, N. Yi Mok, Suzanne Norval, Ruth Brenk, Alan H. Fairlamb, Julie A. Frearson, Kevin D. Read, Ian H. Gilbert, Paul G. Wyatt
This paper is available in a repository.
This paper is available in a repository.

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Abstract

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 EC(50) 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.