Design, synthesis and biological evaluation of bambuterol analogues as novel inhibitors of butyrylcholinesterase.
Eur J Med Chem
; 126: 61-71, 2017 Jan 27.
Article
en En
| MEDLINE
| ID: mdl-27744187
ABSTRACT
An increase activity of butyrylcholinesterase is believed to contribute to Alzheimer's disease. Bambuterol is a known potent inhibitor of butyrylcholinesterase, but it has undesired cardiac effects and less lipophilicity. Thirteen bambuterol analogues were synthesized using 1-(3, 5-dihydroxyphenyl) ethanone as a starting material. In-vitro cholinesterase assay established that the majority of the compounds are specific butyrylcholinesterase inhibitors. Out of the 13 compounds, two bambuterol derivatives, BD-6 and BD-11 exhibited similar efficacies in inhibiting butyrylcholinesterase with fewer effects on heart and enhanced possibilities of permeating through the blood-brain barrier as compared to bambuterol. These bambuterol analogues may provide better alternatives for treatments of Alzheimer's disease.
Palabras clave
Texto completo:
1
Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Terbutalina
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Butirilcolinesterasa
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Diseño de Fármacos
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Inhibidores de la Colinesterasa
Límite:
Adult
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Animals
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Humans
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Male
Idioma:
En
Revista:
Eur J Med Chem
Año:
2017
Tipo del documento:
Article