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http://hdl.handle.net/10773/20399
Título: | In vitro efficiency of 9-(N-cinnamoylbutyl)aminoacridines against blood- and liver-stage malaria parasites |
Autor: | Perez, Bianca Teixeira, Catia Gomes, Ana S. Albuquerque, Ines S. Gut, Jiri Rosenthal, Philip J. Prudencio, Miguel Gomes, Paula |
Palavras-chave: | RESISTANT PLASMODIUM-FALCIPARUM CHLOROQUINE DISCOVERY LEADS |
Data: | 2013 |
Editora: | PERGAMON-ELSEVIER SCIENCE LTD |
Resumo: | Novel 9-aminoacridine derivatives were synthesized by linking the heteroaromatic core to different cinnamic acids through an aminobutyl chain. The test compounds demonstrated mid-nanomolar in vitro activity against erythrocytic stages of the chloroquine-resistant W2 strain of the human malaria parasite Plasmodium falciparum. Two of the most active derivatives also showed in vitro activity against liver-stage Plasmodium berghei, with activity greater than that of the reference liver-stage antimalarial primaquine. The compounds were not toxic to human hepatoma cells at concentrations up to 5 mu M. Hence, 9-(N-cinnamoylbutyl)aminoacridines are a new class of leads for prevention and treatment of malaria. (c) 2012 Elsevier Ltd. All rights reserved. |
Peer review: | yes |
URI: | http://hdl.handle.net/10773/20399 |
DOI: | 10.1016/j.bmcl.2012.12.032 |
ISSN: | 0960-894X |
Versão do Editor: | 10.1016/j.bmcl.2012.12.032 |
Aparece nas coleções: | CICECO - Artigos |
Ficheiros deste registo:
Ficheiro | Descrição | Tamanho | Formato | |
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In vitro efficiency of 9-(N-cinnamoylbutyl)aminoacridines against blood- and liver-stage malaria parasites_10.1016j.bmcl.2012.12.032.pdf | 293.49 kB | Adobe PDF |
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