title: Glycosyl hydroperoxides: a new class of potential antimalarial agents.
abstract: Motivated by the antimalarial properties observed in organic peroxides, an extensive series of glycosyl hydroperoxides was prepared with the aim of identifying new bioactive molecules. Selected compounds were tested against a Plasmodium falciparum culture (chloroquine-susceptible strain D10 and chloroquine-resistant strain W2). Screening results indicated that the factors critical for antimalarial activity were the presence of a hydroperoxide moiety and solubility in water at pH 5.0. Moreover, the ability to inhibit β-hematin formation in vitro has been evaluated (BHIA Assay).
authors.affiliation: Institute of Organic Chemistry of the Polish Academy of Sciences, Kasprzaka 44/52, 01-224 Warsaw, Poland.
authors.forename: Barbara
authors.initials: B
authors.lastname: Szechner
authors.affiliation: Department of Lipids and Liposomes, Faculty of Biotechnology, University of Wroclaw, Joliot-Curie 14A, 50-383 Wroclaw, Poland.
authors.forename: Anna
authors.initials: A
authors.lastname: Jaromin
authors.affiliation: Dipartimento di Scienze Farmacologiche e Biomolecolari, Università degli Studi di Milano, Via Pascal, 36 Milan, Italy.
authors.forename: Silvia
authors.initials: S
authors.lastname: Parapini
authors.affiliation: Dipartimento di Scienze Biomediche, Chirurgiche e Odontoiatriche, Università degli Studi di Milano, Via Pascal, 36 Milan, Italy.
authors.forename: Nicoletta
authors.initials: N
authors.lastname: Basilico
authors.affiliation: Institute of Organic Chemistry of the Polish Academy of Sciences, Kasprzaka 44/52, 01-224 Warsaw, Poland.
authors.forename: Barbara
authors.initials: B
authors.lastname: Grzeszczyk
authors.affiliation: Institute of Organic Chemistry of the Polish Academy of Sciences, Kasprzaka 44/52, 01-224 Warsaw, Poland.
authors.forename: Bartłomiej
authors.initials: B
authors.lastname: Furman
authors.affiliation: Institute of Organic Chemistry of the Polish Academy of Sciences, Kasprzaka 44/52, 01-224 Warsaw, Poland. Electronic address: marek.chmielewski@icho.edu.pl.
authors.forename: Marek
authors.initials: M
authors.lastname: Chmielewski
mesh_terms: D000962:Antimalarials / Q000138:chemical synthesis* / Q000494:pharmacology; D002738:Chloroquine / Q000494:pharmacology; D004912:Erythrocytes / Q000187:drug effects / Q000469:parasitology / Q000473:pathology; D006027:Glycosides / Q000138:chemical synthesis* / Q000494:pharmacology; D006420:Hemeproteins / Q000037:antagonists & inhibitors* / Q000096:biosynthesis; D006801:Humans; D006863:Hydrogen-Ion Concentration; D021261:Parasitic Sensitivity Tests; D010545:Peroxides / Q000138:chemical synthesis* / Q000494:pharmacology; D010963:Plasmodium falciparum / Q000187:drug effects* / Q000254:growth & development; D012995:Solubility; D013045:Species Specificity; D013329:Structure-Activity Relationship
chemical_list: D000962:Antimalarials; D006027:Glycosides; D006420:Hemeproteins; D010545:Peroxides; C020753:hemozoin; D002738:Chloroquine
keywords: Antimalarial compounds; Glycosides; Hydroperoxides