title: In vitro activities of piperaquine and other 4-aminoquinolines against clinical isolates of Plasmodium falciparum in Cameroon.
abstract: The spread of chloroquine-resistant Plasmodium falciparum calls for a constant search for new drugs. The in vitro activity of piperaquine, a new Chinese synthetic drug belonging to the bisquinolines, was evaluated in 103 fresh clinical isolates of P. falciparum in Cameroon, Central Africa, and compared with that of other 4-aminoquinoline and Mannich base derivatives and dihydroartemisinin. Piperaquine was highly active (geometric mean 50% inhibitory concentration, 38.9 nmol/liter; range, 7.76 to 78.3 nmol/liter) and equally active (P > 0.05) against the chloroquine-sensitive and the chloroquine-resistant isolates. There was a significant but low correlation of response between chloroquine and piperaquine (r = 0.257, P < 0.05). These results suggest that further development of piperaquine, in combination with dihydroartemisinin, holds promise for use in chloroquine-resistant regions of endemicity.
authors.affiliation: Unité de Recherche Paludologie Afro-tropicale, Institut de Recherche pour le Développement (IRD), Organisation de Coordination pour la lutte contre les Endémies en Afrique Centrale (OCEAC), Yaoundé, Cameroon. lkbasco@yahoo.fr
authors.forename: Leonardo K
authors.initials: LK
authors.lastname: Basco
authors.forename: Pascal
authors.initials: P
authors.lastname: Ringwald
mesh_terms: D000634:Aminoquinolines / Q000494:pharmacology*; D000818:Animals; D000962:Antimalarials / Q000494:pharmacology*; D002163:Cameroon; D002738:Chloroquine / Q000494:pharmacology; D004351:Drug Resistance; D006801:Humans; D010963:Plasmodium falciparum / Q000187:drug effects*; D011804:Quinolines / Q000494:pharmacology*; D010879:Piperazines
chemical_list: D000634:Aminoquinolines; D000962:Antimalarials; D002738:Chloroquine; D011804:Quinolines; C034759:piperaquine; D010879:Piperazines