title: Synthesis and evaluation of non-peptidic cysteine protease inhibitors of P. falciparum derived from etacrynic acid.
abstract: 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.
authors.affiliation: Research Center for Infectious Diseases, University of Würzburg, Röntgenring 11, 97070 Würzburg, Germany. adrienne.dude@uni-wuerzburg.de
authors.forename: Marie-Adrienne
authors.initials: MA
authors.lastname: Dude
authors.forename: Ulrich
authors.initials: U
authors.lastname: Kaeppler
authors.forename: Monika
authors.initials: M
authors.lastname: Herb
authors.forename: Markus
authors.initials: M
authors.lastname: Schiller
authors.forename: Franziska
authors.initials: F
authors.lastname: Schulz
authors.forename: Birgit
authors.initials: B
authors.lastname: Vedder
authors.forename: Saskia
authors.initials: S
authors.lastname: Heppner
authors.forename: Gabriele
authors.initials: G
authors.lastname: Pradel
authors.forename: Jiri
authors.initials: J
authors.lastname: Gut
authors.forename: Philip J
authors.initials: PJ
authors.lastname: Rosenthal
authors.forename: Tanja
authors.initials: T
authors.lastname: Schirmeister
authors.forename: Matthias
authors.initials: M
authors.lastname: Leippe
authors.forename: Christoph
authors.initials: C
authors.lastname: Gelhaus
mesh_terms: D000818:Animals; D000962:Antimalarials / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D003546:Cysteine Endopeptidases / Q000187:drug effects* / Q000235:genetics; D015853:Cysteine Proteinase Inhibitors / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D004976:Ethacrynic Acid / Q000031:analogs & derivatives*; D015394:Molecular Structure; D010963:Plasmodium falciparum / Q000187:drug effects* / Q000201:enzymology; D011994:Recombinant Proteins / Q000037:antagonists & inhibitors / Q000235:genetics
chemical_list: D000962:Antimalarials; D015853:Cysteine Proteinase Inhibitors; D011994:Recombinant Proteins; D003546:Cysteine Endopeptidases; C416224:falcipain 2; C443101:falcipain 3; D004976:Ethacrynic Acid