7399-04-4Relevant academic research and scientific papers
Novel squaramides with in vitro liver stage antiplasmodial 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)
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.
8-Aminoquinolines as anticoccidials - Part III
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)
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.
