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...
| Main Authors: | , , , , , , , , , , , , |
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| Format: | Article |
| Language: | English |
| Published: |
MDPI AG
2008-12-01
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| Series: | Molecules |
| Subjects: | |
| Online Access: | http://www.mdpi.com/1420-3049/14/1/19/ |
| _version_ | 1819242648764940288 |
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| author | 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 |
| author_facet | 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 |
| author_sort | Christoph Gelhaus |
| collection | DOAJ |
| 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 IC50 values of 9.0 and 18.8 μM against Plasmodia. |
| first_indexed | 2024-12-23T14:43:09Z |
| format | Article |
| id | doaj.art-4565cec2b0ab47c490c6d71ee08fe49e |
| institution | Directory Open Access Journal |
| issn | 1420-3049 |
| language | English |
| last_indexed | 2024-12-23T14:43:09Z |
| publishDate | 2008-12-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Molecules |
| spelling | doaj.art-4565cec2b0ab47c490c6d71ee08fe49e2022-12-21T17:43:10ZengMDPI AGMolecules1420-30492008-12-01141193510.3390/molecules14010019Synthesis and Evaluation of Non-peptidic Cysteine Protease Inhibitors of P. falciparum Derived from Etacrynic AcidChristoph GelhausMatthias LeippeTanja SchirmeisterPhilip J. RosenthalJiri GutGabriele PradelSaskia HeppnerBirgit VedderFranziska SchulzMarkus SchillerMonika HerbUlrich KaepplerMarie-Adrienne DudeA 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.http://www.mdpi.com/1420-3049/14/1/19/MalariaCysteine protease inhibitorEtacrynic acid |
| spellingShingle | 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 Synthesis and Evaluation of Non-peptidic Cysteine Protease Inhibitors of P. falciparum Derived from Etacrynic Acid Molecules Malaria Cysteine protease inhibitor 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 | Malaria Cysteine protease inhibitor Etacrynic acid |
| url | http://www.mdpi.com/1420-3049/14/1/19/ |
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