Novel 2-phenoxyanilide congeners derived from a hit structure of the TCAMS: Synthesis and evaluation of their in vitro activity against plasmodium falciparum

Thomas Weidner, Abed Nasereddin, Lutz Preu, Johann Grünefeld, Ron Dzikowski, Conrad Kunick

Research output: Contribution to journalArticlepeer-review

Abstract

The Tres Cantos Antimalarial Compound Set (TCAMS) is a publicly available compound library which contains 13533 hit structures with confirmed activity against Plasmodium falciparum, the infective agent responsible for malaria tropica. The TCAMS provides a variety of starting points for the investigation of new antiplasmodial drug leads. One of the promising compounds is TCMDC-137332, which seemed to be a good starting point due to its antiplasmodial potency and its predicted physicochemical properties. Several new analogues based on a 2-phenoxyanilide scaffold were synthesized by standard amide coupling reactions and were fully characterized regarding their identity and purity by spectroscopic and chromatographic methods. Furthermore, the results of the biological evaluation of all congeners against Plasmodium falciparum NF54 strains are presented. The findings of our in vitro screening could not confirm the presumed nanomolar antiplasmodial activity of TCMDC-137332 and its derivatives.

Original languageAmerican English
Article number223
JournalMolecules
Volume21
Issue number2
DOIs
StatePublished - 1 Feb 2016

Keywords

  • 2-phenoxyanilide
  • Diarylether
  • Luciferase
  • Malaria
  • Plasmodium falciparum
  • TCAMS
  • TCMDC-137332

All Science Journal Classification (ASJC) codes

  • Analytical Chemistry
  • Chemistry (miscellaneous)
  • Molecular Medicine
  • Pharmaceutical Science
  • Drug Discovery
  • Physical and Theoretical Chemistry
  • Organic Chemistry

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