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

Autor:	Monika Herb, Tanja Schirmeister, Matthias Leippe, Ulrich Kaeppler, Philip J. Rosenthal, Markus Schiller, Saskia Heppner, Marie-Adrienne Dude, Franziska Schulz, Gabriele Pradel, Birgit Vedder, Jiri Gut, Christoph Gelhaus
Rok vydání:	2008
Předmět:	Etacrynic acid Plasmodium falciparum Pharmaceutical Science Cysteine Proteinase Inhibitors Article Analytical Chemistry lcsh:QD241-441 Medicinal and Biomolecular Chemistry Antimalarials Rare Diseases lcsh:Organic chemistry Malaria Cysteine protease inhibitor Theoretical and Computational Chemistry Drug Discovery parasitic diseases medicine Animals Physical and Theoretical Chemistry biology Molecular Structure Extramural Chemistry Organic Chemistry Cysteine proteinases biology.organism_classification Cysteine protease In vitro Recombinant Proteins Vector-Borne Diseases Cysteine Endopeptidases Orphan Drug Ethacrynic Acid Biochemistry Chemistry (miscellaneous) 5.1 Pharmaceuticals Molecular Medicine Development of treatments and therapeutic interventions medicine.drug
Zdroj:	Molecules Molecules; Volume 14; Issue 1; Pages: 19-35 Molecules, Vol 14, Iss 1, Pp 19-35 (2008) Molecules (Basel, Switzerland), vol 14, iss 1
ISSN:	1420-3049
DOI:	10.3390/molecules14010019
Popis:	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.
Databáze:	OpenAIRE
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