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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Veröffentlicht in:	Molecules (Basel, Switzerland) Switzerland), 2008-12, Vol.14 (1), p.19-35
Hauptverfasser:	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:	Artikel
Sprache:	eng
Schlagworte:	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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Zusammenfassung:	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