title: Synthesis and antimalarial activity of urenyl Bis-chalcone in vitro and in vivo.
abstract: Some novel derivatives of Bis-chalcone were synthesized and characterized by their physical and spectral data. All the synthesized compounds were subsequently screened for in vitro globin hydrolysis, β-hematin formation, and murine Plasmodium berghei, using chloroquine as the reference drug. Most of the synthesized compounds exhibited mild to moderate susceptibilities toward the parasite in comparison with the standard. The most active antimalarial compound was 1,1-Bis-[(3',4'-N-(urenylphenyl)-3-(3″,4″,5″-trimethoxyphenyl)]-2-propen-1-one 5, with a percentage of inhibition of heme polymerization of 87.05 ± 0.77, and this compound increased the survival time after infection, reduce the parasitemia and delay the progression of malaria.
authors.affiliation: Laboratorio de Síntesis Orgánica, Facultad de Farmacia, Universidad Central de Venezuela , Caracas 1051 , Venezuela.
authors.forename: José N
authors.initials: JN
authors.lastname: Domínguez
authors.forename: Neira Gamboa
authors.initials: NG
authors.lastname: de Domínguez
authors.forename: Juan
authors.initials: J
authors.lastname: Rodrigues
authors.forename: María Eugenia
authors.initials: ME
authors.lastname: Acosta
authors.forename: Noris
authors.initials: N
authors.lastname: Caraballo
authors.forename: Caritza
authors.initials: C
authors.lastname: León
mesh_terms: D000818:Animals; D000962:Antimalarials / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D047188:Chalcones / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D006418:Heme / Q000037:antagonists & inhibitors / Q000138:chemical synthesis / Q000737:chemistry; D008297:Male; D051379:Mice; D008815:Mice, Inbred Strains; D015394:Molecular Structure; D021261:Parasitic Sensitivity Tests; D010962:Plasmodium berghei / Q000187:drug effects*; D058105:Polymerization / Q000187:drug effects; D013329:Structure-Activity Relationship
chemical_list: D000962:Antimalarials; D047188:Chalcones; D006418:Heme