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

Bioorganic & medicinal chemistry letters (2013-01-08)
Bianca Pérez, Cátia Teixeira, Ana S Gomes, Inês S Albuquerque, Jiri Gut, Philip J Rosenthal, Miguel Prudêncio, Paula Gomes
ABSTRACT

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 μM. Hence, 9-(N-cinnamoylbutyl)aminoacridines are a new class of leads for prevention and treatment of malaria.

MATERIALS
Product Number
Brand
Product Description

Sigma-Aldrich
Cinnamoyl chloride, ≥95.0%