1174155-00-0Relevant articles and documents
Synthesis and Evaluation of Non-peptidic Cysteine Protease Inhibitors of P. falciparum Derived from Etacrynic Acid
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
experimental part, p. 19 - 35 (2009/09/08)
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.