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, 28 (14), 2485-2489

1,2-Diphenoxiethane Salts as Potent Antiplasmodial Agents


1,2-Diphenoxiethane Salts as Potent Antiplasmodial Agents

Santiago Schiafino-Ortega et al. Bioorg Med Chem Lett.


In this article we present a series of non-cytotoxic potent human choline kinase (CK) inhibitors that exhibit nanomolar antiplasmodial activity in vitro. The most active antiplasmodial compounds, 10a-b, bearing a pyridinium cationic head were inactive against CK, while compounds 10g and 10j with a quinolinium moiety exhibit moderate inhibition of both the parasite and the enzyme. The results point towards an additional mechanism of action unrelated to CK inhibition that remains to be established.

Keywords: Antiplasmodial agents; Non-cytotoxic; Plasmodium falciparum.

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