Artemisinin-dipeptidyl vinyl sulfone hybrid molecules
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 fa...
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| Outros Autores: | , , , , , , |
| Formato: | article |
| Idioma: | eng |
| Publicado em: |
2015
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| Assuntos: | |
| Texto completo: | http://hdl.handle.net/10451/21198 |
| País: | Portugal |
| Oai: | oai:repositorio.ul.pt:10451/21198 |
| Resumo: | 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.. - FCT (Portugal) [SFRH/BD/30418/2006]; National Institutes of Health. - This work was supported by FCT (Portugal) and the National Institutes of Health; R. C. acknowledges FCT for the PhD grant SFRH/BD/30418/2006. PJR is a Doris Duke Charitable Foundation Distinguished Clinical Scientist. |
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