Synthesis, trypanocidal activity and molecular modeling studies of 2-alkylaminomethylquinoline derivatives
- Muscia, Gisela Celeste
- Cazorla, Silvia Ines
- Frank, Fernanda Maria
- Borosky, Gabriela Leonor
- Buldain, Graciela Yolanda
- Asís, Sivlia E.
- Malchiodi, Emilio Luis
DOIAbstract
Research and development of new drugs effective in the treatment of Trypanosoma cruzi infections are a real need for the 16 million people infected in the Americas. In a previous work, a quinoline derivative substituted by a 2-piperidylmethyl moiety showed to be active against Chagas disease and was considered a lead compound for further optimization. A series of ten analogous derivatives were tested against epimastigotes as a first approach. In view of their promising results, six of them were evaluated against the blood and intracellular replicative forms of the parasite in humans. Among them, compound 12 which possesses a 6-acetamidohexylamino substituent showed remarkable improvement in activity against epimastigotes, trypomastigotes an...
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