Synthesis and acetylcholinesterase/butyrylcholinesterase inhibition activity of new tacrine-like analogues

The synthesis and preliminary results for acetylcholinesterase and butyrylcholinesterase inhibition activity of a series of pyrano[2,3-b]quinolines (2, 3) and benzonaphthyridines (5, 6) derivatives are described. These molecules are tacrine-like analogues which have been prepared from readily availa...

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Detalhes bibliográficos
Autor principal: Marco, JL (author)
Outros Autores: de los Rios, C (author), Carreiras, MC (author), Banos, JE (author), Badia, A (author), Vivas, NM (author)
Formato: article
Idioma:eng
Publicado em: 2015
Assuntos:
Biochemistry & Molecular Biology
Chemistry, Medicinal
Chemistry, Organic
Texto completo:http://hdl.handle.net/10451/21378
País:Portugal
Oai:oai:repositorio.ul.pt:10451/21378
Descrição
Resumo:The synthesis and preliminary results for acetylcholinesterase and butyrylcholinesterase inhibition activity of a series of pyrano[2,3-b]quinolines (2, 3) and benzonaphthyridines (5, 6) derivatives are described. These molecules are tacrine-like analogues which have been prepared from readily available polyfunctionalized ethyl [6-amino-5-cyano-4H-pyrans and 6-amino-5-cyanopyridine s]-3-carboxylates via Friedlander condensation with selected ketone s. These compounds showed moderate acetylcholinesterase inhibition activity, the more potent (2e, 5b) being 6 times less active than tacrine. The butyrylcholinesterase activity of some of these molecules is also discussed. (C) 2001 Elsevier Science Ltd. All rights reserved.

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