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

• Type: Article in International Scientific Journal
• Date: 2013

Authors

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

Journal

Title: Bioorganic and Medicinal Chemistry Letters

Vol. 23

Pages: 610-613

ISSN: 0960-894X

Publisher: Elsevier

Indexing

ISI Web of Knowledge - 34 Citations

Scopus - 37 Citations

Scientific classification

FOS: Medical and Health sciences > Health sciences

Other information

Authenticus ID: 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.

Language: English

Type (Professor's evaluation): Scientific