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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| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2742655 | PMC |
| http://dx.doi.org/10.1016/j.bmcl.2009.04.100 | DOI Listing |
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