Letters in Drug Design & Discovery

G. Perry
University of Texas
San Antonio, TX
USA
Email: lddd@benthamscience.org

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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, Patricia Escobar Rivero.

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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Article Details

VOLUME: 4
ISSUE: 4
Year: 2007
Page: [293 - 296]
Pages: 4
DOI: 10.2174/157018007784620031
Price: $58