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Biological Activity of Sym-Triazines With Acetylcholine-Like Substitutions as Multitarget Modulators of Alzheimer's Disease

Biological Activity of Sym-Triazines With Acetylcholine-Like Substitutions as Multitarget Modulators of Alzheimer's Disease

Anthony J Veloso, Ari M Chow, Devjani Dhar, Derek W F Tang, Hashwin V S Ganesh, Svetlana Mikhaylichenko, Ian R Brown, Kagan Kerman

ACS Chem Neurosci. 2013 Jun 19;4(6):924-9.

PMID: 23472585

Abstract:

The bioactivities of two novel compounds (TAE-1 and TAE-2) that contain a sym-triazine scaffold with acetylcholine-like substitutions are examined as promising candidate agents against Alzheimer's disease. Inhibition of amyloid-β fibril formation in the presence of Aβ1-42, evaluated by Thioflavin T fluorescence, demonstrated comparable or improved activity to a previously reported pentapeptide-based fibrillogenesis inhibitor, iAβ5p. Destabilization of Aβ1-42 assemblies by TAE-1 and TAE-2 was confirmed by scanning electron microscopy imaging. sym-Triazine inhibition of acetylcholinesterase (AChE) activity was observed in cytosol extracted from differentiated human SH-SY5Y neuronal cells and also using human erythrocyte AChE. The sym-triazine derivatives were well tolerated by these cells and promoted beneficial effects on human neurons, upregulating expression of synaptophysin, a synaptic marker protein, and MAP2, a neuronal differentiation marker.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP1414469592	TAE-1		1414469-59-2	Price

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