Drug intelligence / Profile preview

TACRINE(8)-4-AMINOQUINOLINE

Development stage
Preclinical
Modality
Small Molecules
01

Overview

TACRINE(8)-4-AMINOQUINOLINE is an experimental small molecule hybrid compound that combines structural features of tacrine (a known acetylcholinesterase inhibitor) and 4-aminoquinoline. It belongs to the acridine class of organic compounds. This hybrid was designed to act as a multifunctional agent for potential treatment of neurodegenerative diseases such as Alzheimer's disease. Its mechanism includes potent inhibition of both acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE), with higher potency than tacrine alone. Additionally, it may inhibit β‑amyloid aggregation promoted by AChE and possesses antioxidant properties as well as metal-chelating activity—particularly for copper ions—which are relevant in neuroprotection and reduction of oxidative stress in the brain[5][2][6]. The compound is not approved for clinical use.

Other names
N-quinolin-4-yl-N'-(1,2,3,4-tetrahydroacridin-9-yl)octane-1,8-diamineN1-(quinolin-4-yl)-N8-(1,2,3,4-tetrahydroacridin-9-yl)octane-1,8-diamineN-{8-[1,2,3,4-tetrahydroacrid–9–yl]amino}octyl}quinolin–4–amine
02

Targets

AcetylcholinesteraseAcetylcholinesterase peripheral anionic siteButyrylcholinesteraseAmyloid-beta aggregate (N-terminal epitope)

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