Synthesis and biological evaluation of potential acetylcholinesterase inhibitors based on a benzoxazine core
| Primer Autor |
Mendez-Rojas, Claudio
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| Co-autores |
Quiroz, Gabriel#Faundez, Mario#Gallardo-Garrido, Carlos#David Pessoa-Mahana, C.#Chung, Hery#Gallardo-Toledo, Eduardo#Saitz-Barria, Claudio#Araya-Maturana, Ramiro#Kogan, Marcelo J.#Zuniga-Lopez, Maria C.#Iturriaga-Vasquez, Patricio#Valenzuela-Gutierrez, Carla#Pessoa-Mahana, Hernan
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| Título |
Synthesis and biological evaluation of potential acetylcholinesterase inhibitors based on a benzoxazine core
|
| Editorial |
WILEY-V C H VERLAG GMBH
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| Revista |
ARCHIV DER PHARMAZIE
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| Lenguaje |
en
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| Resumen |
With the purpose of expanding the structural variety of chemical compounds available as pharmacological tools for the treatment of Alzheimer's disease, we synthesized and evaluated a novel series of indole-benzoxazinones (Family I) and benzoxazine-arylpiperazine derivatives (Family II) for potential human acetylcholinesterase (hAChE) inhibitory properties. The most active compounds 7a and 7d demonstrated effective inhibitory profiles with K-i values of 20.3 +/- 0.9 mu M and 20.2 +/- 0.9 mu M, respectively. Kinetic inhibition assays showed non-competitive inhibition of AChE by the tested compounds. According to our docking studies, the most active compounds from both series (Families I and II) showed a binding mode similar to donepezil and interact with the same residues.
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| Tipo de Recurso |
Artículo original
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| Description |
FONDECYT, Grant numbers: 1130347, 1170269, 1150615
FONDECYT, Números de subvención: 1130347, 1170269, 1150615
|
| doi |
10.1002/ardp.201800024
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| Formato Recurso |
pdf
|
| Palabras Claves |
Alzheimer's disease# benzoxazinones# human acetylcholinesterase inhibition# indole
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| Ubicación del archivo |
http://dx.doi.org/10.1002/ardp.201800024
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| Categoría OCDE |
Chemistry, Medicinal# Chemistry, Multidisciplinary# Pharmacology & Pharmacy
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| Materias |
enfermedad de Alzheimer# benzoxazinonas# inhibición de la acetilcolinesterasa humana# indol
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| Disciplinas de la OCDE |
Química Orgánica
Farmacología y Farmacia
Otros Temas de Medicina Clínica
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| Id de Web of Science |
WOS:000431489000009
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| Título de la cita (Recomendado-único) |
Synthesis and biological evaluation of potential acetylcholinesterase inhibitors based on a benzoxazine core
|
| Identificador del recurso (Mandatado-único) |
Artículo original
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| Versión del recurso (Recomendado-único) |
version publicada
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| Editorial |
WILEY-V C H VERLAG GMBH
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| Revista/Libro |
ARCHIV DER PHARMAZIE
|
| Categoría WOS |
Química Medicinal# Química Multidisciplinaria# Farmacología y farmacia
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| ISSN |
0365-6233
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| Idioma |
en
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| Referencia del Financiador (Mandatado si es aplicable-repetible) |
ANID FONDECYT 1130347#ANID FONDECYT 1170269#ANID FONDECYT 1150615
ANID FONDECYT 1130347
ANID FONDECYT 1170269
ANID FONDECYT 1150615
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| Descripción |
FONDECYT, Grant numbers: 1130347, 1170269, 1150615
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| Formato |
pdf
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| Tipo de ruta |
hibrida
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| Access Rights |
metadata
|
| Derechos de acceso |
metadata
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| Página de inicio (Recomendado-único) |
292
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| Página final (Recomendado-único) |
298
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