Metachloridine-substituted Aryl Biguanides as Possible Antimalarial Compounds

METANILAMIDES are reported to have no antibacterial action 1 , 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 metachloridine 3 ( SN 11437) (2-metanilamido-5-chloropyrimidine), which has been found to be effective both in avian 3 and human malarias 4,5,6 . Metachloridine is 5-chloropyrimidine-substituted metanilamide, the action of which is not affected by the presence of p -aminobenzoic acid, and is supposed 3 to have a double mode of action due to the presence of 5-chloropyrimidine and metanilamide parts in the molecule.