Target-Oriented Synthesis of Antiparasitic 2-Hetaryl Substituted Quinolines Based on Imino Diels-Alder Reactions

Title: Target-Oriented Synthesis of Antiparasitic 2-Hetaryl Substituted Quinolines Based on Imino Diels-Alder Reactions

Volume: 4 Issue: 4

Author(s): Vladimir V. Kouznetsov, Leonor Y. Vargas Mendez, Sandra Milena Leal, Uriel Mora Cruz, Carlos Andres Coronado, Carlos M. Melendez Gomez, Arnold R. Romero Bohorquez and Patricia Escobar Rivero

Affiliation:

Keywords: Antiparasitic activities, Target-oriented synthesis, 2-hetarylquinolines, Leishmania chagasi, Trypanosoma cruzi, Drug discovery

Abstract: 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.

Cite this article as:

Kouznetsov V. Vladimir, Vargas Mendez Y. Leonor, Milena Leal Sandra, Mora Cruz Uriel, Andres Coronado Carlos, Melendez Gomez M. Carlos, Romero Bohorquez R. Arnold and Escobar Rivero Patricia, Target-Oriented Synthesis of Antiparasitic 2-Hetaryl Substituted Quinolines Based on Imino Diels-Alder Reactions, Letters in Drug Design & Discovery 2007; 4 (4) . https://dx.doi.org/10.2174/157018007784620031