Abstract
Derivatives of boromycin, which has significant antimalarial properties both in vitro and in vivo, were examined for similar the efficacy against both drug-resistance strain and drug-sensitive strain of malaria and as a means to elucidate structure-activity relationships. More potent in vitro compounds tended to lose their properties in vivo when administered orally. Some novel 16-O-acyl derivatives were found to be more potent and selective antimalarial compounds compared to boromycin. Furthermore, alkyne-bearing 16-O-alkylacyl compounds retained reasonably good efficacy in vivo when given per os.
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