Synthesis and Characterization of Tetrahydroquinolines as Acetylcholinesterase Inhibitors.

Gutierrez, M.; Arevalo, B.; Valdes, F.; Martinez, G.; Vallejos, G.; Carmona, U.; Astudillo, L

Keywords: acetylcholinesterase, tetrahydroquinolines, Povarov Reaction

Abstract

Quinoline is a heterocyclic scaffold of paramount importance to human race. Quinolines and their derivatives occur in numerous natural resources. Compounds containing quinoline structure are widely used as antiasthmatic, antimalarials, anti-viral, anti-inflammatory, antibacterials, antifungals, and anticancer (1). Among quinoline derivatives, tetrahydroquinolines (THQs) are an important structural subunit of natural and synthetic products and many THQs derivatives exhibit interesting biological and pharmaceutical activities (2). Many quinoline derivatives have shown anti-cholinesterase activity and can be potential agents for treatment of Alzheimer disease (3-5).In the present study we have synthesized 7 derivatives of THQs with different patterns of substituent using the Povarov reaction in presence of Lewis acid, all compounds was characterized by 1H-NMR, 13C-NMR and Mass Spectra, and evaluated as potentials inhibitors of acetylcholinesterase.

Más información

Título de la Revista: In Proceedings of the 17th Int. Electron. Conf. Synth. Org. Chem.
Volumen: 17
Fecha de publicación: 2013
Página de inicio: 1
Página final: 30
Idioma: Inglés