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Synthesis and Antimalarial Activity of Mallatojaponin C and Related Compounds
Alexander L Eaton1, Seema Dalal1, M Belen Cassera1
1Department of Chemistry and the Virginia Tech Center for Drug Discovery and ‡Department of Biochemistry and the Virginia Tech Center for Drug Discovery, Virginia Tech , Blacksburg, Virginia 24061, United States.
Abstract:
The phloroglucinol mallotojaponin C (1) from Mallotus oppositifolius, which was previously shown by us to have both antiplasmodial and cytocidal activities against the malaria parasite Plasmodium falciparum, was synthesized in three steps from 2',4',6'-trihydroxyacetophenone, and various derivatives were synthesized in an attempt to improve the bioactivity of this class of compounds. Two derivatives, the simple prenylated phloroglucinols 12 and 13, were found to have comparable antiplasmodial activities to that of mallotojaponin C.
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