title: Evaluation of substituted phenalenone analogues as antiplasmodial agents.
abstract: A set of derivatives encompassing structural modifications on the privileged phenalenone scaffold were assessed for their antiplasmodial activities against a strain of chloroquine sensitive Plasmodium falciparum F32. Two compounds exhibited considerable effects against the malaria parasite (IC₅₀ ≤ 1 μg/mL), one of which maintained the same level of activity in a chloroquine-resistant strain. This is the first record of antiplasmodial activity on this type of scaffold, providing a new structural motif as a new lead for antimalarial activity.
authors.affiliation: Instituto de Investigaciones Fármaco Bioquímicas, Facultad de Ciencias Farmacéuticas y Bioquímicas, Universidad Mayor de San Andrés, Avenida Saavedra 2224, Miraflores, La Paz, Bolivia.
authors.forename: David
authors.initials: D
authors.lastname: Gutiérrez
authors.forename: Ninoska
authors.initials: N
authors.lastname: Flores
authors.forename: Teresa
authors.initials: T
authors.lastname: Abad-Grillo
authors.forename: Grant
authors.initials: G
authors.lastname: McNaughton-Smith
mesh_terms: D000962:Antimalarials / Q000737:chemistry / Q000494:pharmacology*; D002738:Chloroquine / Q000494:pharmacology; D004912:Erythrocytes / Q000469:parasitology; D006801:Humans; D020128:Inhibitory Concentration 50; D043803:Phenalenes / Q000737:chemistry* / Q000494:pharmacology*; D010963:Plasmodium falciparum / Q000187:drug effects*
chemical_list: D000962:Antimalarials; D043803:Phenalenes; C038036:phenalen-1-one; D002738:Chloroquine
keywords: Antiplasmodial; P. falciparum; Substituted phenalenones