Development of a highly-specific
Acta Pharmaceutica Sinica B
; (6): 1686-1695, 2021.
Article
em En
| WPRIM
| ID: wpr-888829
Biblioteca responsável:
WPRO
ABSTRACT
As a serine hydrolase, monoacylglycerol lipase (MAGL) is principally responsible for the metabolism of 2-arachidonoylglycerol (2-AG) in the central nervous system (CNS), leading to the formation of arachidonic acid (AA). Dysfunction of MAGL has been associated with multiple CNS disorders and symptoms, including neuroinflammation, cognitive impairment, epileptogenesis, nociception and neurodegenerative diseases. Inhibition of MAGL provides a promising therapeutic direction for the treatment of these conditions, and a MAGL positron emission tomography (PET) probe would greatly facilitate preclinical and clinical development of MAGL inhibitors. Herein, we design and synthesize a small library of fluoropyridyl-containing MAGL inhibitor candidates. Pharmacological evaluation of these candidates by activity-based protein profiling identified
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Base de dados:
WPRIM
Idioma:
En
Revista:
Acta Pharmaceutica Sinica B
Ano de publicação:
2021
Tipo de documento:
Article