2-Arylpaullones are selective antitrypanosomal agents

Jasmin Ryczak, Ma'ayan Papini, Annette Lader, Abedelmajeed Nasereddin, Dmitry Kopelyanskiy, Lutz Preu, Charles L. Jaffe*, Conrad Kunick

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

25 Scopus citations

Abstract

Antileishmanial paullone-chalcone hybrid molecules display antiparasitic activity against Trypanosoma brucei rhodesiense blood stream forms, albeit with low selectivity against human THP-1 cells. In order to develop less toxic analogues, paullones with acrylamide or aryl substituents in 2-position were synthesized, of which the latter exhibited potent antiparasitic activity with excellent selectivity profiles. The most potent compound identified in this study was 9-tert-butyl-2-(4-morpholinophenyl)paullone (3i) which inhibited the parasites at submicromolar concentrations (GI50 = 510 nM) with a selectivity index of 157.

Original languageEnglish
Pages (from-to)396-400
Number of pages5
JournalEuropean Journal of Medicinal Chemistry
Volume64
DOIs
StatePublished - 2013

Keywords

  • Neglected tropical diseases
  • Paullones
  • Suzuki reaction
  • Trypanosoma brucei rhodesiense
  • Trypanosomiasis

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