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

…, R Oliveira, LM Gonçalves, A Domingos, J Gut…

Index: Capela, Rita; Oliveira, Rudi; Goncalves, Lidia M.; Domingos, Ana; Gut, Jiri; Rosenthal, Philip J.; Lopes, Francisca; Moreira, Rui Bioorganic and Medicinal Chemistry Letters, 2009 , vol. 19, # 12 p. 3229 - 3232

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Citation Number: 37

Abstract

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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