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Molecules 2009, 14(1), 19-35;

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

Research Center for Infectious Diseases, University of Würzburg, Röntgenring 11, 97070 Würzburg, Germany
Institute of Pharmacy and Food Chemistry, Am Hubland, D-97074 Würzburg, Germany
Zoological Institute, University of Kiel, Olshausenstr. 40, D-24098 Kiel, Germany
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
(This article belongs to the Special Issue Neglected Diseases: Medicinal Chemistry and Natural Product Chemistry)
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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. View Full-Text
Keywords: Malaria; Cysteine protease inhibitor; Etacrynic acid Malaria; Cysteine protease inhibitor; Etacrynic acid

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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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