Molecules (Dec 2008)

Synthesis and Evaluation of Non-peptidic Cysteine Protease Inhibitors of P. falciparum Derived from Etacrynic Acid

  • Christoph Gelhaus,
  • Matthias Leippe,
  • Tanja Schirmeister,
  • Philip J. Rosenthal,
  • Jiri Gut,
  • Gabriele Pradel,
  • Saskia Heppner,
  • Birgit Vedder,
  • Franziska Schulz,
  • Markus Schiller,
  • Monika Herb,
  • Ulrich Kaeppler,
  • Marie-Adrienne Dude

DOI
https://doi.org/10.3390/molecules14010019
Journal volume & issue
Vol. 14, no. 1
pp. 19 – 35

Abstract

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A series of etacrynic acid derivatives was synthesized and screened for their in vitro activity against Plasmodium falciparum, as well as their activity against recombinantly expressed falcipain-2 and -3. The two most active compounds of the series displayed IC50 values of 9.0 and 18.8 μM against Plasmodia.

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