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1,2-Diphenoxiethane salts as potent antiplasmodial agents. | LitMetric

1,2-Diphenoxiethane salts as potent antiplasmodial agents.

Bioorg Med Chem Lett

Departamento de Química Farmacéutica y Orgánica, Facultad de Farmacia, Campus de Cartuja, 18071 Granada, Spain. Electronic address:

Published: August 2018

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.

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http://dx.doi.org/10.1016/j.bmcl.2018.05.060DOI Listing

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