Bis-(4-aminophenyl)-sulfone and several N,N'-diacyl derivatives have shown appreciable activity as antimalarials. With the assumption that a molecule more readily cleaved to a p-aminophenyl sulfur or oxidized sulfur anion, as a potential anti-PAB substance, might be a more effective antimalarial, a series of N,N',-diacyl derivatives of bis-(4-aminophenyl) disulfide was synthesized. Oxidation with peroxide followed by acylation gave the corresponding thiolsulfinates. Antimalarial activity was found for bis-(4-p-acetamidobenzenesulfonamidophenyl) disulfide and N,N′-bis-(α-aminoacyl) derivatives of bis-(4-aminophenyl)-sulfone.

Bis-(4-aminophenyl) disulfide and its thiolsulfinate show antimalarial activity, suggesting potential as anti-PAB substances.

Paper

N-acyl derivatives of bis-(4-aminophenyl) disulfide and its thiolsulfinate.

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