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

作者：Capela Rita; Oliveira Rudi; Goncalves Lidia M; Domingos Ana; Gut Jiri; Rosenthal Philip J; Lopes Francisca^*; Moreira Rui

来源：Bioorganic & Medicinal Chemistry Letters, 2009, 19(12): 3229-3232.

DOI：10.1016/j.bmcl.2009.04.100

• Antimalarial
• Artemisinin
• FP-2
• Vinylsulfone

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.

• 出版日期2009-6-15