Rapid discovery and crystallography study of highly potent and selective butylcholinesterase inhibitors based on oxime-containing libraries and conformational restriction strategies

Keywords

Alzheimer's disease

Butylcholinesterase inhibitors

Combinatorial chemistry

Conformational restriction

Microscale synthesis

AbbreviationsBuChE

butyrylcholinesterase

PAS

peripheral anionic site

CuAAC

Copper-catalysed azide–alkyne cycloadditions

Cdc25

Cell division cycle 25

HIV

human immunodeficiency virus

HATU

2-(7-aza-1H-benzotriazole-1-yl)-1,1,3,3-tetramethyluronium hexafluorophosphate

EDC·HCl

1-(3-Dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride

TLC

thin-layer chromatography

APP

amyloid precursor protein

CNS

central nervous system

PAMPA

parallel artificial membrane permeability assay

Data availability

Data will be made available on request.

© 2023 Elsevier Inc. All rights reserved.

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