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 μM against...

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Autores principales: 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
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Molecular Diversity Preservation International 2008
Materias:
Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6253875/
https://www.ncbi.nlm.nih.gov/pubmed/19104483
http://dx.doi.org/10.3390/molecules14010019
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author 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
author_facet 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
author_sort Dude, Marie-Adrienne
collection PubMed
description 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 μM against Plasmodia.
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spelling pubmed-62538752018-11-30 Synthesis and Evaluation of Non-peptidic Cysteine Protease Inhibitors of P. falciparum Derived from Etacrynic Acid 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 Molecules Article 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 μM against Plasmodia. Molecular Diversity Preservation International 2008-12-23 /pmc/articles/PMC6253875/ /pubmed/19104483 http://dx.doi.org/10.3390/molecules14010019 Text en © 2009 by the authors; licensee Molecular Diversity Preservation International, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution license (http://creativecommons.org/licenses/by/3.0/).
spellingShingle Article
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
Synthesis and Evaluation of Non-peptidic Cysteine Protease Inhibitors of P. falciparum Derived from Etacrynic Acid
title Synthesis and Evaluation of Non-peptidic Cysteine Protease Inhibitors of P. falciparum Derived from Etacrynic Acid
title_full Synthesis and Evaluation of Non-peptidic Cysteine Protease Inhibitors of P. falciparum Derived from Etacrynic Acid
title_fullStr Synthesis and Evaluation of Non-peptidic Cysteine Protease Inhibitors of P. falciparum Derived from Etacrynic Acid
title_full_unstemmed Synthesis and Evaluation of Non-peptidic Cysteine Protease Inhibitors of P. falciparum Derived from Etacrynic Acid
title_short Synthesis and Evaluation of Non-peptidic Cysteine Protease Inhibitors of P. falciparum Derived from Etacrynic Acid
title_sort synthesis and evaluation of non-peptidic cysteine protease inhibitors of p. falciparum derived from etacrynic acid
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6253875/
https://www.ncbi.nlm.nih.gov/pubmed/19104483
http://dx.doi.org/10.3390/molecules14010019
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