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ABSTRACT:
SUBMITTER: Qiu GL
PROVIDER: S-EPMC6179045 | biostudies-literature | 2018 Dec
REPOSITORIES: biostudies-literature
Journal of enzyme inhibition and medicinal chemistry 20181201 1
Based on the structural analysis of tricyclic scaffolds as butyrylcholinesterase (BuChE) inhibitors, a series of pyrazolo[1,5-c][1,3]benzoxazin-5(5H)-one derivatives were designed, synthesized and evaluated for their acetylcholinesterase (AChE) and BuChE inhibitory activity. Compounds with 5-carbonyl and 7- or/and 9-halogen substitutions showed potential BuChE inhibitory activity, among which compounds 6a, 6c and 6g showed the best BuChE inhibition (IC<sub>50</sub> = 1.06, 1.63 and 1.63 µM, resp ...[more]