Detalhes bibliográficos
| 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. |
| Autores principais: | Perez, Bianca |
| Outros Autores: | Teixeira, Catia; Gomes, Ana S.; Albuquerque, Ines S.; Gut, Jiri; Rosenthal, Philip J.; Prudencio, Miguel; Gomes, Paula |
| Assunto: | RESISTANT PLASMODIUM-FALCIPARUM CHLOROQUINE DISCOVERY LEADS |
| Ano: | 2013 |
| País: | Portugal |
| Tipo de documento: | artigo |
| Tipo de acesso: | acesso restrito |
| Instituição associada: | Universidade de Aveiro |
| Idioma: | inglês |
| Origem: | RIA - Repositório Institucional da Universidade de Aveiro |