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

Marie-Adrienne Dude 1 email, Ulrich Kaeppler 2 , Monika Herb 2 , Markus Schiller 2 , Franziska Schulz 3 , Birgit Vedder 3 , Saskia Heppner 3 , Gabriele Pradel 1 email, Jiri Gut 4 , Philip J. Rosenthal 4 email, Tanja Schirmeister 2 email, Matthias Leippe 3 email and Christoph Gelhaus 3,* email
1 Research Center for Infectious Diseases, University of Würzburg, Röntgenring 11, 97070 Würzburg, Germany 2 Institute of Pharmacy and Food Chemistry, Am Hubland, D-97074 Würzburg, Germany 3 Zoological Institute, University of Kiel, Olshausenstr. 40, D-24098 Kiel, Germany 4 Department of Medicine, San Francisco General Hospital, University of California, San Francisco, CA 94143-0811, USA
* Author to whom correspondence should be addressed.
Received: 20 November 2008; in revised form: 12 December 2008 / Accepted: 19 December 2008 / Published: 23 December 2008
(This article belongs to the Special Issue Neglected Diseases: Medicinal Chemistry and Natural Product Chemistry)
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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

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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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