Artículo
Alkynyl and β-ketophosphonates: Selective and potent butyrylcholinesterase inhibitors
Fecha de publicación:
04/2018
Editorial:
Academic Press Inc Elsevier Science
Revista:
Bioorganic Chemistry
ISSN:
0045-2068
Idioma:
Inglés
Tipo de recurso:
Artículo publicado
Clasificación temática:
Resumen
A series of thirty-three alkynyl and β-ketophosphonates were evaluated for their in vitro acetyl- and butyryl-cholinesterase (AChE and BChE) inhibitory activities using Ellman´s spectrophotometric method. None of the examined compounds inhibited AChE activity at tested concentrations while twenty-nine of them showed significant and selective inhibition of BChE with IC50 values between 38.60 µM and 0.04 µM. In addition, structure-activity relationships were discussed. The most effective inhibitors were the dibutyl o-methoxyphenyl alkynylphosphonate 3dc and dibutyl o-methoxyphenyl β-ketophosphonate 4dc. Activities of most potent compounds were also compared with a commercial organophosphorus compound. These results could inspire the design of new inhibitors with stronger activity against BChE.
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Articulos(INQUISUR)
Articulos de INST.DE QUIMICA DEL SUR
Articulos de INST.DE QUIMICA DEL SUR
Citación
Cavallaro, Valeria; Moglie, Yanina Fernanda; Murray, Ana Paula; Radivoy, Gabriel Eduardo; Alkynyl and β-ketophosphonates: Selective and potent butyrylcholinesterase inhibitors; Academic Press Inc Elsevier Science; Bioorganic Chemistry; 77; 4-2018; 420-428
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