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(S)-tacrine(10)-hupyridone

Development stage
Preclinical
Modality
Small Molecules
01

Overview

(S)-tacrine(10)-hupyridone is a synthetic small molecule designed as a dual-binding acetylcholinesterase inhibitor. It incorporates a tacrine moiety linked via a decyl chain to a hupyridone fragment. Tacrine is known as a reversible cholinesterase inhibitor; the addition of the hupyridone group enhances binding affinity and selectivity for acetylcholinesterase. This compound was developed to improve potency and reduce side effects compared to tacrine alone. Preclinical studies have shown that it inhibits acetylcholinesterase in a mixed competitive manner with high potency and can reverse cognitive impairments in animal models of Alzheimer's disease by crossing the blood-brain barrier and reducing brain AChE activity[6][8][9].

Other names
(5S)-5-{[10-(1,2,3,4-tetrahydroacridin-9-yl)amino]decyl}amino-5,6,7,8-tetrahydroquinolin-2(1H)-one(S)-N-9-(1,2,3,4-tetrahydroacridinyl)-N'-5-[5,6,7,8-tetrahydro-2'(1'H)-quinolinonyl]-1,10-diaminodecane
02

Targets

Acetylcholinesterase

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