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

Molecules

Marie-Adrienne Dude²  Ulrich Kaeppler³  Monika Herb³  Markus Schiller³  Birgit Vedder³  Saskia Heppner¹  Gabriele Pradel²  Jiri Gut⁴  Philip J. Rosenthal⁴  Tanja Schirmeister³  Matthias Leippe¹ 

[1] Zoological Institute, University of Kiel, Olshausenstr. 40, D-24098 Kiel, GermanyE-mail:;Research Center for Infectious Diseases, University of Würzburg, Röntgenring 11, 97070 Würzburg, Germany; E-mail:;Institute of Pharmacy and Food Chemistry, Am Hubland, D-97074 Würzburg, Germany E-mail:;Department of Medicine, San Francisco General Hospital, University of California, San Francisco, CA 94143-0811, USA; E-mail:

关键词: Malaria;    Cysteine protease inhibitor;    Etacrynic acid.;   

DOI  :  10.3390/molecules14010019

来源: mdpi

【 摘 要 】

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.

【 授权许可】

CC BY   
© 2009 by the authors; licensee Molecular Diversity Preservation International, Basel, Switzerland.