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

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

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Authors

  • Victoria C. Smith
  • Laura A. T. Cleghorn
  • Andrew Woodland
  • Daniel Spinks
  • Irene Hallyburton
  • Iain T. Collie
  • N. Yi Mok
  • Suzanne Norval
  • Ruth Brenk
  • Alan H. Fairlamb
  • Julie A. Frearson
  • Kevin D. Read
  • Ian H. Gilbert
  • Paul G. Wyatt

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Info

Original languageEnglish
Pages1832-1840
Number of pages9
JournalChemMedChem
Journal publication date4 Oct 2011
Volume6
Issue10
DOIs
StatePublished

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 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.

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