Experimental and Theoretical Approaches in the Study of Phenanthroline-Tetrahydroquinolines for Alzheimer's Disease

Yorley Duarte, Margarita Gutierrez, Rocío Álvarez, Jans H. Alzate-Morales, Jorge Soto-Delgado

Resultado de la investigación: Article

Resumen

The imino-Diels-Alder reaction is one of the most common strategies in organic chemistry and is an important tool for providing a broad spectrum of biologically active heterocyclic systems. A combined theoretical and experimental study of the imino-Diels-Alder reaction is described. The new phenanthroline-tetrahydroquinolines were evaluated as cholinesterase inhibitors. Their cytotoxicity in human neuroblastoma SH-SY5Y cells was also evaluated. The theoretical results suggest that compounds formation in stages can be explained by endo cycloadducts under the established reaction conditions, thereby confirming experimental results obtained for percentage yield. These results allowed us to establish that pyridine substituent remarkably influences activation energy and reaction yield, as well as in acetylcholinesterase (AChE) activity. Among these derivatives, compounds with 4-pyridyl and 4-nitrophenyl showed favorable AChE activity and proved to be non-cytotoxic.

Idioma originalEnglish
Páginas (desde-hasta)627-636
Número de páginas10
PublicaciónChemistryOpen
Volumen8
N.º5
DOI
EstadoPublished - 1 may 2019

Huella dactilar

Phenanthrolines
Acetylcholinesterase
Cholinesterase Inhibitors
Cytotoxicity
Activation energy
Chemical activation
Derivatives
1,2,3,4-tetrahydroquinoline
Organic Chemistry
4-nitrophenyl
pyridine

ASJC Scopus subject areas

  • Chemistry(all)

Citar esto

Duarte, Yorley ; Gutierrez, Margarita ; Álvarez, Rocío ; Alzate-Morales, Jans H. ; Soto-Delgado, Jorge. / Experimental and Theoretical Approaches in the Study of Phenanthroline-Tetrahydroquinolines for Alzheimer's Disease. En: ChemistryOpen. 2019 ; Vol. 8, N.º 5. pp. 627-636.
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Experimental and Theoretical Approaches in the Study of Phenanthroline-Tetrahydroquinolines for Alzheimer's Disease. / Duarte, Yorley; Gutierrez, Margarita; Álvarez, Rocío; Alzate-Morales, Jans H.; Soto-Delgado, Jorge.

En: ChemistryOpen, Vol. 8, N.º 5, 01.05.2019, p. 627-636.

Resultado de la investigación: Article

TY - JOUR

T1 - Experimental and Theoretical Approaches in the Study of Phenanthroline-Tetrahydroquinolines for Alzheimer's Disease

AU - Duarte, Yorley

AU - Gutierrez, Margarita

AU - Álvarez, Rocío

AU - Alzate-Morales, Jans H.

AU - Soto-Delgado, Jorge

PY - 2019/5/1

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