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

doi:10.3390/molecules14010019

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

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

Marie-Adrienne Dude ¹ , Ulrich Kaeppler ², Monika Herb ², Markus Schiller ², Franziska Schulz ³, Birgit Vedder ³, Saskia Heppner ³, Gabriele Pradel ¹ , Jiri Gut ⁴, Philip J. Rosenthal ⁴ , Tanja Schirmeister ² , Matthias Leippe ³ and Christoph Gelhaus ³^,*

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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Cite This Article

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 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(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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