Novel squaramides with in vitro liver stage antiplasmodial activity
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.
Ribeiro, Carlos J.A.,Espadinha, Margarida,Machado, Marta,Gut, Jiri,Gon?alves, Lídia M.,Rosenthal, Philip J.,Prudêncio, Miguel,Moreira, Rui,Santos, Maria M.M.
p. 1786 - 1792
(2016/04/05)
8-Aminoquinolines as anticoccidials - Part III
Analogues of the antimalarial pentaquine, 1, in which the nature of the side-chain on the 8-amino position was varied, were prepared and evaluated for anticoccidial activity both in vitro and in vivo. Specifically, both the inter-nitrogen distance and the nature of the terminal amino group were investigated. Novel analogues of equal or improved efficacy in vitro and in vivo to pentaquine were discovered.
Armer, Richard E.,Barlow, Jacqueline S.,Chopra, Narinder,Dutton, Christopher J.,Greenway, David H.J.,Greenwood, Sean D.W.,Lad, Nita,Shaw, Jonothan,Thompson, Adrian P.,Thong, Kam-Wah,Tommasini, Ivan
p. 2425 - 2430
(2007/10/03)
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