title: Plasmepsin II inhibition and antiplasmodial activity of Primaquine-Statine 'double-drugs'.
abstract: Statine-based inhibitors of Plasmepsin II (PLMII) coupled with Primaquine have been designed using the 'double-drug' approach. The IC50 values for PLMII inhibition ranged from 0.59 to 400 nM and the best IC50 value for inhibition of Plasmodium falciparum growth in vitro was 0.4 microM, which represent a remarkable improvement compared to other statine-based PLMII inhibitors.
authors.affiliation: Institute of Medicinal Chemistry, University of Milan, Viale Abruzzi 42, 20131 Milan, Italy. sergio.romeo@unimi.it
authors.forename: Sergio
authors.initials: S
authors.lastname: Romeo
authors.forename: Mario
authors.initials: M
authors.lastname: Dell'Agli
authors.forename: Silvia
authors.initials: S
authors.lastname: Parapini
authors.forename: Luca
authors.initials: L
authors.lastname: Rizzi
authors.forename: Germana
authors.initials: G
authors.lastname: Galli
authors.forename: Monica
authors.initials: M
authors.lastname: Mondani
authors.forename: Anna
authors.initials: A
authors.lastname: Sparatore
authors.forename: Donatella
authors.initials: D
authors.lastname: Taramelli
authors.forename: Enrica
authors.initials: E
authors.lastname: Bosisio
mesh_terms: D000596:Amino Acids / Q000737:chemistry* / Q000494:pharmacology; D000818:Animals; D000962:Antimalarials / Q000138:chemical synthesis* / Q000494:pharmacology; D016282:Aspartic Acid Endopeptidases / Q000037:antagonists & inhibitors*; D002738:Chloroquine; D003432:Cross-Linking Reagents; D015195:Drug Design; D004351:Drug Resistance; D004912:Erythrocytes / Q000382:microbiology; D006801:Humans; D020128:Inhibitory Concentration 50; D010963:Plasmodium falciparum / Q000187:drug effects* / Q000201:enzymology; D011319:Primaquine / Q000737:chemistry* / Q000494:pharmacology; D011480:Protease Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D015800:Protozoan Proteins; D013329:Structure-Activity Relationship
chemical_list: D000596:Amino Acids; D000962:Antimalarials; D003432:Cross-Linking Reagents; D011480:Protease Inhibitors; D015800:Protozoan Proteins; D002738:Chloroquine; D016282:Aspartic Acid Endopeptidases; C100637:plasmepsin II; D011319:Primaquine; C013165:statine