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 IC(50) values of 9.0 and 18.8 microM agai...

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Bibliographic Details
Published in:Molecules (Basel, Switzerland) Switzerland), 2008-12, Vol.14 (1), p.19-35
Main Authors: 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
Format: Article
Language:English
Subjects:
Acids
Animals
Antimalarials - chemical synthesis
Antimalarials - chemistry
Antimalarials - pharmacology
Cysteine Endopeptidases - drug effects
Cysteine Endopeptidases - genetics
Cysteine protease inhibitor
Cysteine Proteinase Inhibitors - chemical synthesis
Cysteine Proteinase Inhibitors - chemistry
Cysteine Proteinase Inhibitors - pharmacology
Etacrynic acid
Ethacrynic Acid - analogs & derivatives
Hemoglobin
Malaria
Molecular Structure
Parasites
Plasmodium falciparum - drug effects
Plasmodium falciparum - enzymology
Recombinant Proteins - antagonists & inhibitors
Recombinant Proteins - genetics
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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 IC(50) values of 9.0 and 18.8 microM against Plasmodia.
ISSN:1420-3049
1420-3049
DOI:10.3390/molecules14010019