Novel squaramides with in vitro liver stage antiplasmodial activity

Publication date: Available online 3 March 2016
Source:Bioorganic & Medicinal Chemistry
Author(s): Carlos J.A. Ribeiro, Margarida Espadinha, Marta Machado, Jiri Gut, Lídia M. Gonçalves, Philip J. Rosenthal, Miguel Prudêncio, Rui Moreira, Maria M. M. Santos
A structure-activity relationship study was performed with ten 8-aminoquinoline-squaramides compounds active against liver stage malaria parasites, using human hepatoma cells (Huh7) infected by Plasmodium berghei parasites. In addition, their blood-schizontocidal activity was assessed against chloroquine-resistant W2 strain Plasmodium falciparum. Compound 3 was 7.3-fold more potent than the positive control primaquine against liver-stage parasites, illustrating the importance of the squarate moiety to activity.

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