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

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

2, 2, 2, 3, 3, 3, 1
4, 4
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 / Revised: 12 December 2008 / Accepted: 19 December 2008 / Published: 23 December 2008
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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.
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 (CC BY 3.0).

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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.

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