In vitro efficiency of 9-(N-cinnamoylbutyl)aminoacridines against blood- and liver-stage malaria parasites

• Tipo: Artigo em Revista Científica Internacional
• Data: 2013

Autores

Bianca Perez (Autor) Outra; Catia Teixeira (Autor) Outra; Ana S Gomes (Autor) Outra; Ines S Albuquerque (Autor) Outra; Jiri Gut (Autor) Outra; Philip J Rosenthal (Autor) Outra; Miguel Prudencio (Autor) Outra; Paula Gomes (Autor) FCUP

Revista

Título: Bioorganic and Medicinal Chemistry Letters

Vol. 23

Páginas: 610-613

ISSN: 0960-894X

Editora: Elsevier

Indexação

ISI Web of Knowledge - 34 Citações

Scopus - 37 Citações

Classificação Científica

FOS: Ciências médicas e da saúde > Ciências da saúde

Outras Informações

ID Authenticus: P-002-0YN

DOI: 10.1016/j.bmcl.2012.12.032

Abstract (EN): 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.

Idioma: Inglês

Tipo (Avaliação Docente): Científica