Utilize este identificador para referenciar este registo: http://hdl.handle.net/10451/3860
Título: Design, synthesis and evaluation of 3-methylene-substituted indolinones as antimalarials
Autor: Kumar, S. Praveen
Gut, Jiri
Guedes, Rita C.
Rosenthal, Philip J.
Santos, Maria M. M.
Moreira, Rui
Palavras-chave: Indolin-2-ones
Falcipain inhibitor
Antiplasmodial activity
Malaria
Data: 2011
Editora: Elsevier
Citação: 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.
Resumo: 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.
Peer review: yes
URI: http://dx.doi.org/10.1016/j.ejmech.2011.01.008
http://hdl.handle.net/10451/3860
ISSN: 0223-5234
Versão do Editor: http://www.sciencedirect.com/science/article/pii/S022352341100016X
Aparece nas colecções:FF - Artigos em Revistas Internacionais

Ficheiros deste registo:
Ficheiro Descrição TamanhoFormato 
versao_online_(3).pdf297,86 kBAdobe PDFVer/Abrir    Acesso Restrito. Solicitar cópia ao autor!


FacebookTwitterDeliciousLinkedInDiggGoogle BookmarksMySpace
Formato BibTex MendeleyEndnote Degois 

Todos os registos no repositório estão protegidos por leis de copyright, com todos os direitos reservados.