Correlation of antimalarial activity of artemisinin derivatives with binding affinity with ferroprotoporphyrin IX.

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Paitayatat S, Tarnchompoo B, Thebtaranonth Y, Yuthavong Y

Correlation of antimalarial activity of artemisinin derivatives with binding affinity with ferroprotoporphyrin IX.

J Med Chem. 1997 Feb 28;40(5):633-8. doi: 10.1021/jm960767v.

PubMed ID
9057849 [ View in PubMed
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Abstract

The antimalarial activity of a number of artemisinin derivatives, both newly synthesized and currently used as drugs, against Plasmodium falciparum in culture shows a correlation with their affinity of binding with ferroprotoporphyrin IX, as measured from the spectral change of the latter. The new C-16-functionalized artemisinin derivatives were obtained through a novel one-pot synthesis of artemisitene (2) from naturally abundant artemisinin (1), followed by Michael addition with nucleophiles. The correlation points to the biological significance of the interaction of these derivatives with ferroprotoporphyrin IX and may provide a basis for primary screening of peroxidic antimalarials of similar structures.

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