Synthesis and biological evaluation of new quinoline derivatives as antileishmanial and antitrypanosomal agents
- Chanquia, Santiago Nahuel
- Larregui, Facundo
- Puente, Vanesa Rocío
- Labriola, Carlos Alberto
- Lombardo, Maria Elisa
- Garcia Liñares, Guadalupe Eugenia
DOIAbstract
As a part of our project aimed at developing new safe chemotherapeutic agents against tropical diseases, a series of aryl derivatives of 2- and 3-aminoquinoline, some of them new compounds, was designed, synthesized, and evaluated as antiproliferative agents against Trypanosoma cruzi, the parasite responsible for American trypanosomiasis (Chagas’ disease), and Leishmania mexicana, the etiological agent of Leishmaniasis. Some of them showed a remarkable activity as parasite growth inhibitors. Fluorine-containing derivatives 11b and 11c were more than twice more potent than geneticin against intracellular promastigote form of Leishmania mexicana exhibiting both IC 50 values of 41.9 μM. The IC 50 values corresponding to fluorine and chlorine d...
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