Antimalarial activities of 25 derivatives of artemisinine against chloroquine-resistant plasmodium berghei

作者: Qu Zx , Gu Hm , Lu Bf

DOI:

关键词: ArtemisininArtemisininsStereochemistryAlpha (ethology)Alkoxy groupBeta (finance)ChemistryStructure–activity relationshipPlasmodium bergheiChloroquine

摘要: The antimalarial activities of 25 derivatives artemisinine, including dihydroartemisinine, 13 ethers, 6 esters and 5 carbonates, were compared. Each compound, dissovlved in tea seed oil, was injected intramuscularly into mice infected with the chloroquine-resistant strain Plasmodium berghei. Adopting SD90 as a comparision criterion, results showed that many much more potent than artemisinine. They are SM224(O-methyl beta) SM241 (butyryl dihydroartmisinine, alpha) SM108 ( propionyl esters, SM242(propoxy carbonyl alpha), SM275( ethoxy alpha+beta), SM223 (ethoxy alpha ) SM 276 phenoxy alpha+beta) carbonates. Their chemical structures values presented Table 1.

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