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1,2-Diphenoxiethane salts as potent antiplasmodial agents |
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| Authors: | Santiago Schiafino-Ortega Eleonora Baglioni Guiomar Pérez-Moreno Pablo Rios Marco Carmen Marco Dolores González-Pacanowska Luis Miguel Ruiz-Pérez María Paz Carrasco-Jiménez Luisa Carlota López-Cara |
| Affiliation: | 1. Departamento de Química Farmacéutica y Orgánica, Facultad de Farmacia, Campus de Cartuja, 18071 Granada, Spain;2. Instituto de Parasitología y Biomedicina “López-Neyra”, Consejo Superior de Investigaciones Científicas, Parque Tecnológico de Ciencias de la Salud, Avenida del Conocimiento 17, 18016 Armilla, Granada, Spain;3. Departamento de Bioquímica y Biología Molecular I, Facultad de Ciencias, Campus Fuentenueva, 18071 Granada, Spain |
| Abstract: | 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 |
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