title: Synthesis and antiplasmodial activity of 3-furyl and 3-thienylquinoxaline-2-carbonitrile 1,4-di-N-oxide derivatives.
abstract: The aim of this study was to identify new compounds active against Plasmodium falciparum based on our previous research carried out on 3-phenyl-quinoxaline-2-carbonitrile 1,4-di-N-oxide derivatives. Twelve compounds were synthesized and evaluated for antimalarial activity. Eight of them showed an IC(50) less than 1 microM against the 3D7 strain. Derivative 1 demonstrated high potency (IC(50)= 0.63 microM) and good selectivity (SI=10.35), thereby becoming a new lead-compound.
authors.affiliation: Unidad de Investigación y Desarrollo de Medicamentos, Centro de Investigación en Farmacobiología Aplicada (CIFA), University of Navarra, 31080 Pamplona, Spain.
authors.forename: Esther
authors.initials: E
authors.lastname: Vicente
authors.forename: Sarah
authors.initials: S
authors.lastname: Charnaud
authors.forename: Emily
authors.initials: E
authors.lastname: Bongard
authors.forename: Raquel
authors.initials: R
authors.lastname: Villar
authors.forename: Asunción
authors.initials: A
authors.lastname: Burguete
authors.forename: Beatriz
authors.initials: B
authors.lastname: Solano
authors.forename: Saioa
authors.initials: S
authors.lastname: Ancizu
authors.forename: Silvia
authors.initials: S
authors.lastname: Pérez-Silanes
authors.forename: Ignacio
authors.initials: I
authors.lastname: Aldana
authors.forename: Livia
authors.initials: L
authors.lastname: Vivas
authors.forename: Antonio
authors.initials: A
authors.lastname: Monge
mesh_terms: D000818:Animals; D000962:Antimalarials / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D016923:Cell Death / Q000187:drug effects; D002460:Cell Line; D003497:Cyclic N-Oxides / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D004351:Drug Resistance / Q000187:drug effects; D009570:Nitriles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D010087:Oxides / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D021261:Parasitic Sensitivity Tests; D010963:Plasmodium falciparum / Q000187:drug effects*; D011810:Quinoxalines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*
chemical_list: C526930:3-thienylquinoxaline-2-carbonitrile 1,4-di-N-oxide; D000962:Antimalarials; D003497:Cyclic N-Oxides; D009570:Nitriles; D010087:Oxides; D011810:Quinoxalines