Antimalarial activity of oxidized starch and cellulose imine derivatives.
With the purpose of screening potential antimalarial agents, oxidized starch imine derivatives of sulfonamides or pyrimidine - derivatives of sulfisoxazole (ML8), sulfameter (ML11) and trimethoprim (ML13) - and oxidized cellulose imine derivatives of dapsone (ML14), sulfadiazine (ML17), sulfamethoxazole (ML18), sulfisoxazole (ML19), sulfamethoxypyridazine (ML20) and sulfameter (ML22) were submitted to in vivo biological assays with mice infected with Plasmodium berghei. Only ML11 was 100% curative in test conditions; ML 17 showed the same effect as its prototype. The drug content in both prodrugs is lower in the applied dose than that used in the original drugs. It can be suggested that the latentiation enhanced the effectiveness of the prototypes.
Departmento de Farmácia, Faculdade de Ciências Farmacêuticas, Universidade de São Paulo, SP, Brazil.
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Ohara
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Sakuda
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Cruz
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Ferreira
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Korolkovas
D000818:Animals; D000962:Antimalarials / Q000737:chemistry / Q000494:pharmacology*; D002482:Cellulose / Q000737:chemistry / Q000494:pharmacology*; D007097:Imines / Q000737:chemistry / Q000494:pharmacology*; D008288:Malaria / Q000188:drug therapy / Q000469:parasitology; D051379:Mice; D010962:Plasmodium berghei; D013213:Starch / Q000031:analogs & derivatives / Q000737:chemistry / Q000494:pharmacology*
D000962:Antimalarials; D007097:Imines; D002482:Cellulose; D013213:Starch