Artemisinin-dipeptidyl vinyl sulfone hybrid molecules: design, synthesis and preliminary SAR for antiplasmodial activity and falcipain-2 inhibition.

Rita Capela,Rudi Oliveira,Lídia M Gonçalves,Ana Domingos,Jiri Gut,Philip J Rosenthal,Francisca Lopes,Rui Moreira

Bioorganic & Medicinal Chemistry Letters（2009）

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摘要

Artemisinin–vinyl sulfone hybrid molecules were active against the Plasmodium falciparum W2 strain in the low nanomolar range and those containing the Leu-hPhe core inhibited falcipain-2 in low micromolar range.

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关键词

Antimalarial,Artemisinin,FP-2,Vinylsulfone

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