Target-Oriented Synthesis of Antiparasitic 2-Hetaryl Substituted Quinolines Based on Imino Diels-Alder Reactions
Vladimir V. Kouznetsov,
Leonor Y. Vargas Mendez,
Sandra Milena Leal,
Uriel Mora Cruz,
Carlos Andres Coronado,
Carlos M. Melendez Gomez,
Arnold R. Romero Bohorquez,
Patricia Escobar Rivero.
Target-oriented synthesis of new substituted 2-hetarylquinolines 6-19 and their in vitro activity against endemic parasites such as Leishmania chagasi and Trypanosoma cruzi are reported. In addition, their cytotoxicities for mammalian Vero cells and THP-1 macrophages cells are assessed. These studies showed that between the new (tetrahydro)quinolines series tested in these assays, the 4-methyl-8-isopropyl-2-(3- pyridinyl)quinoline 15 exhibits the best in vitro response against both live forms of T. cruzi and L. chagasi parasites and displays no cytotoxic activity on mammalian cells.
Keywords: Antiparasitic activities, Target-oriented synthesis, 2-hetarylquinolines, Leishmania chagasi, Trypanosoma cruzi, Drug discovery
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