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Synthesis and Antimalarial Activity of Heterocyclic Alkyl Disulfides, Thiosulfates, and Dithio Acid Derivatives

Based on the antimalarial activity in mice of bis(4‐p‐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 t...

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Bibliographic Details
Published in:Journal of pharmaceutical sciences 1975-02, Vol.64 (2), p.211-216
Main Authors: Foye, William O., Lanzillo, Joseph J., Lowe, Young Hee, Kauffman, Joel M.
Format: Article
Language:English
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Summary:Based on the antimalarial activity in mice of bis(4‐p‐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‐p‐acetamidobenzenesulfonamidophenyl) disulfide, showed curative activity in either a mouse or chick test.
ISSN:0022-3549
1520-6017
DOI:10.1002/jps.2600640204