Publicação
Design, synthesis and evaluation of 3-methylene-substituted indolinones as antimalarials
| dc.contributor.author | Kumar, S. Praveen | |
| dc.contributor.author | Gut, Jiri | |
| dc.contributor.author | Guedes, Rita C. | |
| dc.contributor.author | Rosenthal, Philip J. | |
| dc.contributor.author | Santos, Maria M. M. | |
| dc.contributor.author | Moreira, Rui | |
| dc.date.accessioned | 2011-08-03T12:51:42Z | |
| dc.date.available | 2011-08-03T12:51:42Z | |
| dc.date.issued | 2011 | |
| dc.date.updated | 2011-07-01T14:07:53Z | |
| dc.description.abstract | The design, synthesis and evaluation of 3-methylene-substituted indolinones as falcipain inhibitors and antiplasmodial agents are described. These compounds react readily with thiols via an addition-elimination mechanism, indicating their potential as cysteine protease inhibitors. Several indolinones containing a Leu-i-amyl recognition moiety were found to be moderate inhibitors of the Plasmodium falciparum cysteine protease falcipain-2, but not of the related protease falcipain-3, and displayed antiplasmodial activity against the chloroquine-resistant P. falciparum W2 strain in the low micromolar range. Coupling a 7-chloroquinoline moiety to the 3-methylene-substituted indolinone scaffold led to a significant improvement in antiplasmodial activity. | por |
| dc.identifier.citation | Kumar, S. Praveen; Gut, Jiri; Guedes, Rita C. ; Rosenthal, Philip J.; Santos, Maria M. M.; Moreira, Rui. Design, synthesis and evaluation of 3-methylene-substituted indolinones as antimalarials, European Journal of Medicinal Chemistry, 46, 927-933, 2011. | por |
| dc.identifier.issn | 0223-5234 | |
| dc.identifier.uri | http://dx.doi.org/10.1016/j.ejmech.2011.01.008 | |
| dc.identifier.uri | http://hdl.handle.net/10451/3860 | |
| dc.language.iso | eng | por |
| dc.peerreviewed | yes | por |
| dc.publisher | Elsevier | por |
| dc.relation.publisherversion | http://www.sciencedirect.com/science/article/pii/S022352341100016X | por |
| dc.subject | Indolin-2-ones | por |
| dc.subject | Falcipain inhibitor | por |
| dc.subject | Antiplasmodial activity | por |
| dc.subject | Malaria | por |
| dc.title | Design, synthesis and evaluation of 3-methylene-substituted indolinones as antimalarials | por |
| dc.type | journal article | |
| dspace.entity.type | Publication | |
| oaire.citation.endPage | 933 | por |
| oaire.citation.startPage | 927 | por |
| oaire.citation.title | European Journal of Medicinal Chemistry | por |
| rcaap.rights | restrictedAccess | por |
| rcaap.type | article | por |