ANTI-MALARIAL ACTIVITY IN ANIMALS OF THE OPTICAL ISOMERS OF CHLOROQUINE DIPHOSPHATE

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  • 1 January 1979
    • journal article
    • research article
    • Vol. 30  (3) , 308-312
Abstract
Optically pure d- and l-chloroquine diphosphate were examined for their efficacy against Plasmodium berghei in mice. The d-enantiomer is significantly more effective than the corresponding l-enantiomer, and in subcurative doses the d-enantiomer is also significantly more active than the racemate. This increased activity has no influence upon chloroquine-resistant strains of P. berghei. The LD50 in non-infected mice is higher for the d-enantiomer than for either the racemate or the l-enantiomer when mice were treated orally 1 and 4 times. These differences in efficacy and toxicity between the d- and l-enantiomer of chloroquine are not as pronounced as those found for the enantiomers of many other drugs and these differences are limited to subcurative doses.

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