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Letters in Drug Design & Discovery

Editor-in-Chief

ISSN (Print): 1570-1808
ISSN (Online): 1875-628X

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

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

Volume 4, Issue 4, 2007

Page: [293 - 296] Pages: 4

DOI: 10.2174/157018007784620031

Price: $65

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.

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


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