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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) which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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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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