title: Synthesis and evaluation of phenylequine for antimalarial activity in vitro and in vivo.
abstract: Synthesis of the potent antiplasmodial 4-aminoquinoline, phenylequine (PQ), is reported for the first time. PQ and the two analogues show increased efficacy in moving from the chloroquine sensitive D10 to the chloroquine resistant K1 strain in vitro. The in vivo efficacy of PQ, and salts thereof, have been determined in Plasmodium berghei ANKA and Plasmodium yoelii. Phenylequine hydrochloride has shown an ED(50) of 0.81 in P. yoelii (cf chloroquine ED(50)=1.31).
authors.affiliation: Department of Chemistry, University of Cape Town, Rondebosch 7701, South Africa.
authors.forename: Margaret A L
authors.initials: MA
authors.lastname: Blackie
authors.forename: Vanessa
authors.initials: V
authors.lastname: Yardley
authors.forename: Kelly
authors.initials: K
authors.lastname: Chibale
mesh_terms: D000634:Aminoquinolines / Q000138:chemical synthesis* / Q000494:pharmacology*; D000962:Antimalarials / Q000138:chemical synthesis* / Q000494:pharmacology*; D002460:Cell Line; D004353:Drug Evaluation, Preclinical / Q000379:methods; D006801:Humans; D010963:Plasmodium falciparum / Q000187:drug effects / Q000502:physiology; D010967:Plasmodium yoelii / Q000187:drug effects / Q000502:physiology
chemical_list: D000634:Aminoquinolines; D000962:Antimalarials; C001920:4-aminoquinoline