Utilize este identificador para referenciar este registo: http://hdl.handle.net/10451/17885
Título: Squaric acid/4-aminoquinoline conjugates: novel potent antiplasmodial agents
Autor: Ribeiro, Carlos J. A.
Kumar, S. P.
Gut, Jiri
Gonçalves, Lidia M.
Rosenthal, Philip J.
Moreira, Rui
Santos, Maria M. M.
Palavras-chave: Squaramide
4-Aminoquinoline
Malaria
Hybrid
Antiplasmodial activity
Data: 2013
Editora: Elsevier
Citação: European Journal of Medicinal Chemistry 69 (2013) 365-372
Resumo: We report the synthesis and structure–activity relationship (SAR) analysis of a series of hybrid compounds containing a squaric moiety conjugated with heterocyclic moieties from well-known antimalarials. This novel series of compounds presents improved antiplasmodial activity compared with the squaric derivatives described in our previous work. Three compounds, 8b (IC50 = 99 nM), 8c (IC50 = 95 nM), and 8d (IC50 = 105 nM) had greater in vitro potency than chloroquine 1 (IC50 = 140 nM) against chloroquine resistant Plasmodium falciparum. In addition, they were noncytotoxic against NIH 3T3 and Hek 293T cells.
Peer review: yes
URI: http://hdl.handle.net/10451/17885
DOI: http://dx.doi.org/10.1016/j.ejmech.2013.08.037
Versão do Editor: http://www.sciencedirect.com/science/article/pii/S0223523413005540
Aparece nas colecções:FF - Artigos em Revistas Internacionais

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