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

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Resumo(s)

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.

Descrição

Palavras-chave

Biochemistry & Molecular Biology Chemistry, Medicinal Chemistry, Organic

Contexto Educativo

Citação

BIOORGANIC & MEDICINAL CHEMISTRY. - Vol. 9, n. 3 (MAR 2001), p. 727-732

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Fascículo

Editora

PERGAMON-ELSEVIER SCIENCE LTD

Licença CC