INVESTIGADORES
GARCIA Manuela Emilia
artículos
Título:
Solanocapsine derivatives as potential inhibitors of acetylcholinesterase: Synthesis, molecular docking and biological studies
Autor/es:
GARCÍA MANUELA*; JOSÉ L. BORIONI; VALERIA CAVALLARO; MARCELO PUIATTI; ADRIANA PIERINI; ANA PAULA MURRAY; ALICIA PEÑÉÑORY*
Revista:
STEROIDS
Editorial:
ELSEVIER SCIENCE INC
Referencias:
Lugar: Amsterdam; Año: 2015 vol. 104 p. 95 - 110
ISSN:
0039-128X
Resumen:
The investigation of natural products in medicinal chemistry is essential today. In this context, acetylcholinesterase(AChE) inhibitors comprise one type of the compounds most actively studied in the searchfor an effective treatment of symptoms of Alzheimer?s disease. This work describes the isolation of anatural compound, solanocapsine, the preparation of its chemical derivatives, the evaluation of AChEinhibitory activity, and the structure?activity analysis of relevant cases. The influence of structural variationson the inhibitory potency was carefully investigated by modifying different reactive parts of theparent molecule. A theoretical study was also carried out into the binding mode of representativecompounds to the enzyme through molecular modeling. The biological properties of the series wereinvestigated. Through this study valuable information was obtained of steroidal alkaloid-type compoundsas a starting point for the synthesis of AChE inhibitors.