title: Aza vinyl sulfones: synthesis and evaluation as antiplasmodial agents.
abstract: A series of novel aza vinyl sulfones were designed, synthesized in good yields and evaluated as antiplasmodial agents. Tested compounds did not show activity against papain or the Plasmodium falciparum cysteine protease falcipain-2. However, a number of the new compounds effectively inhibited the in vitro development of P. falciparum. Compounds containing a squaramide group were the most active, with IC(50) values between 0.95 and 4.5 μM, suggesting that these are potential lead compounds for the development of new antimalarial agents.
authors.affiliation: Research Institute for Medicines and Pharmaceutical Sciences (iMed.UL), Faculty of Pharmacy, University of Lisbon, Av. Prof. Gama Pinto, 1649-003 Lisbon, Portugal.
authors.forename: Paulo M C
authors.initials: PM
authors.lastname: Glória
authors.forename: Jiri
authors.initials: J
authors.lastname: Gut
authors.forename: Lídia M
authors.initials: LM
authors.lastname: Gonçalves
authors.forename: Philip J
authors.initials: PJ
authors.lastname: Rosenthal
authors.forename: Rui
authors.initials: R
authors.lastname: Moreira
authors.forename: Maria M M
authors.initials: MM
authors.lastname: Santos
mesh_terms: D000962:Antimalarials / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D003546:Cysteine Endopeptidases / Q000378:metabolism; D004912:Erythrocytes / Q000469:parasitology; D006801:Humans; D020128:Inhibitory Concentration 50; D016778:Malaria, Falciparum / Q000188:drug therapy; D010963:Plasmodium falciparum / Q000187:drug effects* / Q000201:enzymology; D013450:Sulfones / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*
chemical_list: D000962:Antimalarials; D013450:Sulfones; D003546:Cysteine Endopeptidases; C416224:falcipain 2