title: Huprines as a new family of dual acting trypanocidal-antiplasmodial agents.
abstract: A series of 19 huprines has been evaluated for their activity against cultured bloodstream forms of Trypanosoma brucei and Plasmodium falciparum. Moreover, cytotoxicity against rat myoblast L6 cells was assessed for selected huprines. All the tested huprines are moderately potent and selective trypanocidal agents, exhibiting IC(50) values against T. brucei in the submicromolar to low micromolar range and selectivity indices for T. brucei over L6 cells of approximately 15, thus constituting interesting trypanocidal lead compounds. Two of these huprines were also found to be active against a chloroquine-resistant strain of P. falciparum, thus emerging as interesting trypanocidal-antiplasmodial dual acting compounds, but they exhibited little selectivity for P. falciparum over L6 cells.
authors.affiliation: Facultat de Farmàcia, Universitat de Barcelona, Barcelona, Spain.
authors.forename: Julien
authors.initials: J
authors.lastname: Defaux
authors.forename: Marta
authors.initials: M
authors.lastname: Sala
authors.forename: Xavier
authors.initials: X
authors.lastname: Formosa
authors.forename: Carles
authors.initials: C
authors.lastname: Galdeano
authors.forename: Martin C
authors.initials: MC
authors.lastname: Taylor
authors.forename: Waleed A A
authors.initials: WA
authors.lastname: Alobaid
authors.forename: John M
authors.initials: JM
authors.lastname: Kelly
authors.forename: Colin W
authors.initials: CW
authors.lastname: Wright
authors.forename: Pelayo
authors.initials: P
authors.lastname: Camps
authors.forename: Diego
authors.initials: D
authors.lastname: Muñoz-Torrero
mesh_terms: D000634:Aminoquinolines / Q000138:chemical synthesis* / Q000737:chemistry / Q000145:classification / Q000494:pharmacology; D000818:Animals; D000962:Antimalarials / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D002478:Cells, Cultured; D006576:Heterocyclic Compounds, 4 or More Rings / Q000737:chemistry* / Q000145:classification / Q000494:pharmacology; D015394:Molecular Structure; D010963:Plasmodium falciparum / Q000187:drug effects*; D051381:Rats; D014344:Trypanocidal Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D014346:Trypanosoma brucei brucei / Q000187:drug effects*
chemical_list: D000634:Aminoquinolines; D000962:Antimalarials; D006576:Heterocyclic Compounds, 4 or More Rings; D014344:Trypanocidal Agents; C404518:huprine X