Molecules

Synthesis and evaluation of non-peptidic cysteine protease inhibitors of P. falciparum derived from etacrynic acid

…, B Vedder, S Heppner, G Pradel, J Gut, PJ Rosenthal…

Index: Dude, Marie-Adrienne; Kaeppler, Ulrich; Herb, Monika; Schiller, Markus; Schulz, Franziska; Vedder, Birgit; Heppner, Saskia; Pradel, Gabriele; Gut, Jiri; Rosenthal, Philip J.; Schirmeister, Tanja; Leippe, Matthias; Gelhaus, Christoph Molecules, 2009 , vol. 14, # 1 p. 19 - 35

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Citation Number: 11

Abstract

Abstract: 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 IC 50 values of 9.0 and 18.8 μM against Plasmodia.