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Molecules 2009, 14(1), 19-35; doi:10.3390/molecules14010019
Article

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

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Received: 20 November 2008; in revised form: 12 December 2008 / Accepted: 19 December 2008 / Published: 23 December 2008
Download PDF [196 KB, uploaded 18 June 2014]
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 IC50 values of 9.0 and 18.8 μM against Plasmodia.
Keywords: Malaria; Cysteine protease inhibitor; Etacrynic acid Malaria; Cysteine protease inhibitor; Etacrynic acid
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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MDPI and ACS Style

Dude, M.-A.; Kaeppler, U.; Herb, M.; Schiller, M.; Schulz, F.; Vedder, B.; Heppner, S.; Pradel, G.; Gut, J.; Rosenthal, P.J.; Schirmeister, T.; Leippe, M.; Gelhaus, C. Synthesis and Evaluation of Non-peptidic Cysteine Protease Inhibitors of P. falciparum Derived from Etacrynic Acid. Molecules 2009, 14, 19-35.

AMA Style

Dude M-A, Kaeppler U, Herb M, Schiller M, Schulz F, Vedder B, Heppner S, Pradel G, Gut J, Rosenthal PJ, Schirmeister T, Leippe M, Gelhaus C. Synthesis and Evaluation of Non-peptidic Cysteine Protease Inhibitors of P. falciparum Derived from Etacrynic Acid. Molecules. 2009; 14(1):19-35.

Chicago/Turabian Style

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. 2009. "Synthesis and Evaluation of Non-peptidic Cysteine Protease Inhibitors of P. falciparum Derived from Etacrynic Acid." Molecules 14, no. 1: 19-35.


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