With the purpose of obtaining pro-drugs of dapsone and sulfadimethoxine, those chemotherapeutic agents were attached through covalent bonding to starch polymeric dialdehyde (Sumstar-190). The antimalarial activity of the two resulting compounds – the dapsone saccharidic polymer (PS6) and the sulfadimethoxine saccharidic polymer (PS7) – in mice experimentally inoculated with Plasmodium berghei was significantly increased with this molecular modification. Mice infected with malaria and kept without treatment together with others which received different doses of PS6 and PS7 were also partially or totally cured, possibly due to the ingestion of excrements containing the parent chemotherapeutic agents.

Keywords:
Experimental chemotherapy, Experimental malaria, Saccharidic polymers, Pro-drugs, Dapsone, Sulfadimethoxine
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© 1978 S. Karger AG, Basel
1978
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