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

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

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...

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Bibliographic Details
Main Authors: Christoph Gelhaus, Matthias Leippe, Tanja Schirmeister, Philip J. Rosenthal, Jiri Gut, Gabriele Pradel, Saskia Heppner, Birgit Vedder, Franziska Schulz, Markus Schiller, Monika Herb, Ulrich Kaeppler, Marie-Adrienne Dude
Format: Article
Language:English
Published: MDPI AG 2008-12-01
Series:Molecules
Subjects:
Malaria
Cysteine protease inhibitor
Etacrynic acid
Online Access:http://www.mdpi.com/1420-3049/14/1/19/
Description
Summary: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.
ISSN:1420-3049

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