Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 19, Issue 12, Pages 3229-3232Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2009.04.100
Keywords
Antimalarial; Artemisinin; FP-2; Vinylsulfone
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Funding
- FCT (Portugal) [SFRH/BD/30418/2006]
- National Institutes of Health
- Fundação para a Ciência e a Tecnologia [SFRH/BD/30418/2006] Funding Source: FCT
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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. (C) 2009 Elsevier Ltd. All rights reserved.
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