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Metachloridine-substituted Aryl Biguanides as Possible Antimalarial Compounds

Abstract

METANILAMIDES are reported to have no antibacterial action1, and from the parallel nature of the antimalarial and antibacterial properties of sulphanilamides, discouraged research in the field of metanilamides as possible antimalarials. Recently, English et al.2 discovered enhanced antimalarial activity in 2-sulphanilamido-5-chloropyrimidine, and their work resulted in the discovery of metachloridine3 (SN 11437) (2-metanilamido-5-chloropyrimidine), which has been found to be effective both in avian3 and human malarias4,5,6. Metachloridine is 5-chloropyrimidine-substituted metanilamide, the action of which is not affected by the presence of p-aminobenzoic acid, and is supposed3 to have a double mode of action due to the presence of 5-chloropyrimidine and metanilamide parts in the molecule.

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BAMI, H., IYER, B. & GUHA, P. Metachloridine-substituted Aryl Biguanides as Possible Antimalarial Compounds. Nature 162, 146–147 (1948). https://doi.org/10.1038/162146b0

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