Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1372619 | Bioorganic & Medicinal Chemistry Letters | 2009 | 4 Pages |
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.
Graphical abstractArtemisinin–vinyl sulfone hybrid molecules 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.Figure optionsDownload full-size imageDownload as PowerPoint slide
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Rita Capela, Rudi Oliveira, Lídia M. Gonçalves, Ana Domingos, Jiri Gut, Philip J. Rosenthal, Francisca Lopes, Rui Moreira,