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. 2003 Apr;47(4):1391-4.
doi: 10.1128/AAC.47.4.1391-1394.2003.

In vitro activities of piperaquine and other 4-aminoquinolines against clinical isolates of Plasmodium falciparum in Cameroon

Affiliations

In vitro activities of piperaquine and other 4-aminoquinolines against clinical isolates of Plasmodium falciparum in Cameroon

Leonardo K Basco et al. Antimicrob Agents Chemother. 2003 Apr.

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.

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Figures

FIG. 1.
FIG. 1.
Distribution of IC50s for each of the test compounds. PIP, piperaquine; CQ, chloroquine; MDAQ, monodesethylamodiaquine; PND, pyronaridine; DHA, dihydroartemisinin. The dotted line corresponds to the threshold value for in vitro chloroquine resistance (100 nmol/liter).

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