Synthesis and antimalarial activity of heterocyclic alkyl disulfides, thiosulfates, and dithio acid derivatives.
Based on the antimalarial activity in mice of bis(4-rho-acetamidobenzenesulfonamidophenyl) disulfide, a series of N-heterocyclic alkyl disulfides and thiosulfates was synthesized and screened for antimalarial activity. Several related dithio acid dianions and S- blocked derivatives were also screened to provide an indication of the possible role that thiol anions might play in malaria chemotherapy. Activity was limited by toxicity with these compounds, and none of those tested, with the exception of bis(4-rho-acetamidobenzenesulfonamidophenyl) disulfide, showed curative activity in either a mouse or chick test.
D000818:Animals; D000962:Antimalarials / Q000138:chemical synthesis* / Q000627:therapeutic use; D002645:Chickens; D004220:Disulfides / Q000138:chemical synthesis* / Q000627:therapeutic use; D005260:Female; D006168:Guinea Pigs; D008288:Malaria / Q000188:drug therapy; D010084:Oxidation-Reduction; D010962:Plasmodium berghei; D013438:Sulfhydryl Compounds / Q000138:chemical synthesis / Q000627:therapeutic use; D013885:Thiosulfates / Q000138:chemical synthesis* / Q000627:therapeutic use
D000962:Antimalarials; D004220:Disulfides; D013438:Sulfhydryl Compounds; D013885:Thiosulfates