title: Synthesis and in vitro antiprotozoal evaluation of substituted phenalenone analogues.
abstract: A set of derivatives encompassing structural modifications on the privileged phenalenone scaffold were assessed for their antiparasitic activities against the most clinically relevant forms of trypanosomiasis and leishmaniasis. Several compounds exhibited leishmanicidal effects at levels comparable or better than the reference drug pentamidine, while the parent phenalenone was shown to have a level of activity against Trypanosoma cruzi comparable to the marketed drug benznidazole.
authors.affiliation: Instituto Universitario de Bio-Orgánica 'Antonio González', Universidad de La Laguna, La Laguna, Tenerife, Canary Islands, Spain.
authors.forename: Laura I
authors.initials: LI
authors.lastname: Rosquete
authors.forename: M Gabriela
authors.initials: MG
authors.lastname: Cabrera-Serra
authors.forename: José E
authors.initials: JE
authors.lastname: Piñero
authors.forename: Patricia
authors.initials: P
authors.lastname: Martín-Rodríguez
authors.forename: Leandro
authors.initials: L
authors.lastname: Fernández-Pérez
authors.forename: Javier G
authors.initials: JG
authors.lastname: Luis
authors.forename: Grant
authors.initials: G
authors.lastname: McNaughton-Smith
authors.forename: Teresa
authors.initials: T
authors.lastname: Abad-Grillo
mesh_terms: D000981:Antiprotozoal Agents / Q000138:chemical synthesis* / Q000627:therapeutic use / Q000633:toxicity; D045744:Cell Line, Tumor; D006801:Humans; D007896:Leishmaniasis / Q000188:drug therapy; D010419:Pentamidine / Q000627:therapeutic use; D043803:Phenalenes / Q000737:chemistry* / Q000627:therapeutic use / Q000633:toxicity; D014349:Trypanosoma cruzi / Q000187:drug effects; D014352:Trypanosomiasis / Q000188:drug therapy
chemical_list: D000981:Antiprotozoal Agents; D043803:Phenalenes; C038036:phenalen-1-one; D010419:Pentamidine