Publication
Artemisinin-dipeptidyl vinyl sulfone hybrid molecules
| dc.contributor.author | Capela, Rita | |
| dc.contributor.author | Oliveira, Rudi | |
| dc.contributor.author | Goncalves, Lidia M. | |
| dc.contributor.author | Domingos, Ana | |
| dc.contributor.author | Gut, Jiri | |
| dc.contributor.author | Rosenthal, Philip J. | |
| dc.contributor.author | Lopes, Francisca | |
| dc.contributor.author | Moreira, Rui | |
| dc.date.accessioned | 2015-12-30T10:17:41Z | |
| dc.date.available | 2015-12-30T10:17:41Z | |
| dc.date.issued | 2009 | |
| dc.description.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. (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. | |
| dc.format | application/pdf | |
| dc.identifier.citation | BIOORGANIC & MEDICINAL CHEMISTRY LETTERS. - Vol. 19, n. 12 (2009), p. 3229-3232 | |
| dc.identifier.doi | http://dx.doi.org/10.1016/j.bmcl.2009.04.100 | |
| dc.identifier.issn | 0960-894X | |
| dc.identifier.uri | http://hdl.handle.net/10451/21198 | |
| dc.language.iso | eng | |
| dc.publisher | PERGAMON-ELSEVIER SCIENCE LTD | |
| dc.subject | Chemistry, Medicinal | |
| dc.subject | Chemistry, Organic | |
| dc.title | Artemisinin-dipeptidyl vinyl sulfone hybrid molecules | |
| dc.title | Design, synthesis and preliminary SAR for antiplasmodial activity and falcipain-2 inhibition | |
| dc.type | journal article | |
| dspace.entity.type | Publication | |
| oaire.citation.endPage | 3232 | por |
| oaire.citation.startPage | 3229 | por |
| oaire.citation.title | BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | por |
| oaire.citation.volume | Vol. 19 | por |
| rcaap.rights | restrictedAccess | |
| rcaap.type | article |