Abstract
SINCE the discovery of ‘Paludrine’ (proguanil, N1-p-chlorophenyl-N5-isopropyldiguanide) by Curd, Davey and Rose1, considerable evidence has accumulated that this drug probably differs in its mode of action from most other antimalarials. Direct evidence that proguanil is transformed in the animal body into another, more active, compound was provided by Hawking2 and Hawking and Perry3, who showed that proguanil has no action on in vitro cultures of the exo-erythrocytic forms of Plasmodium gallinaceum or on the blood forms of P. cynomolgi, whereas, under similar conditions, serum from animals dosed with the drug has high antimalarial activity.
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References
Curd, Davey and Rose, Ann. Trop. Med. Parasitol., 39, 208 (1945).
Hawking, Nature, 159, 409 (1947).
Hawking and Perry, Brit. J. Pharmacol., 3, 320 (1948).
Birtwell, Curd, Hendry and Rose, J. Chem. Soc., 1650 (1948).
Crounse, J. Org. Chem., 16, 492 (1951).
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CARRINGTON, H., CROWTHER, A., DAVEY, D. et al. A Metabolite of ‘Paludrine’ with High Antimalarial Activity. Nature 168, 1080 (1951). https://doi.org/10.1038/1681080a0
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DOI: https://doi.org/10.1038/1681080a0
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