Alkynyl and β-ketophosphonates: Selective and potent butyrylcholinesterase inhibitors
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-ni...
| Autores: | , , , |
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| Tipo de recurso: | artículo |
| Estado: | Versión publicada |
| Fecha de publicación: | 2018 |
| País: | Argentina |
| Institución: | Consejo Nacional de Investigaciones Científicas y Técnicas |
| Repositorio: | CONICET Digital (CONICET) |
| Idioma: | inglés |
| OAI Identifier: | oai:ri.conicet.gov.ar:11336/91836 |
| Acceso en línea: | http://hdl.handle.net/11336/91836 |
| Access Level: | acceso abierto |
| Palabra clave: | BUTYRYLCHOLINESTERASE ENZYMATIC INHIBITION ORGANOPHOSPHORUS COMPOUNDS PHOSPHONATES https://purl.org/becyt/ford/1.4 https://purl.org/becyt/ford/1 |
| Sumario: | 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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