Artemisinin-dipeptidyl vinyl sulfone hybrid molecules: design, synthesis and preliminary SAR for antiplasmodial activity and falcipain-2 inhibition
R Capela, R Oliveira, LM Gonçalves… - Bioorganic & medicinal …, 2009 - Elsevier
Bioorganic & medicinal chemistry letters, 2009•Elsevier
A series of artemisinin–vinyl sulfone hybrid molecules with the potential to act in the parasite
food vacuole via endoperoxide activation and falcipain inhibition was synthesized and
screened for antiplasmodial activity and falcipain-2 inhibition. All conjugates 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.
food vacuole via endoperoxide activation and falcipain inhibition was synthesized and
screened for antiplasmodial activity and falcipain-2 inhibition. All conjugates 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.
A series of artemisinin–vinyl sulfone hybrid molecules with the potential to act in the parasite food vacuole via endoperoxide activation and falcipain inhibition was synthesized and screened for antiplasmodial activity and falcipain-2 inhibition. All conjugates 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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