INVESTIGADORES
ALZA Natalia Paola
congresos y reuniones científicas
Título:
Semi-Synthetic Analogs of 17-Hydroxycativic Acid and their Biological Evaluation
Autor/es:
ALZA, N.P.; MURRAY, A.P.
Lugar:
Santiago de Compostela
Reunión:
Conferencia; The 17th International Electronic Conference on Synthetic Organic Chemistry; 2013
Resumen:
A new series of analogs of the naturally occurring 17-hydroxycativic acid (1) were synthesized and evaluated as cholinesterase inhibitors. All derivatives have been fully characterized by mono- and bidimensional NMR spectroscopy. The butyrylcholinesterase (BChE) inhibitory activity of the analogs was of the same order of magnitude as that of compound 1 (IC50 = 171.1 microM), while the acetylcholinesterase (AChE) inhibition was not improved by these derivatizations, being 1 the most potent AChE inhibitor of the series (IC50 =21.1 microM). These results suggest that both carboxylic group (C15) and allylic alcohol (C17) could be important for AChE inhibitory activity.