A novel series of tacrine-selegiline hybrids with cholinesterase and monoamine oxidase inhibition activities for the treatment of Alzheimer's disease.

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Lu C, Zhou Q, Yan J, Du Z, Huang L, Li X

A novel series of tacrine-selegiline hybrids with cholinesterase and monoamine oxidase inhibition activities for the treatment of Alzheimer's disease.

Eur J Med Chem. 2013 Apr;62:745-53. doi: 10.1016/j.ejmech.2013.01.039. Epub 2013 Feb 8.

PubMed ID

23454517 [ View in PubMed

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Abstract

A novel series of tacrine-selegiline hybrids was synthesised and evaluated for application as inhibitors of cholinesterase (AChE/BuChE) and monoamine oxidase (MAO-A/B). The results demonstrate that most of the synthesised compounds exhibit high inhibitory activity. Among these compounds, compound 8g provided a good balance of activity towards all targets (with IC50 values of 22.6 nM, 9.37 nM, 0.3724 muM, and 0.1810 muM for AChE, BuChE, MAO-A and MAO-B, respectively). These results indicated that 8g has the potential to be a multi-functional candidate for Alzheimer's disease.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Clorgiline	Amine oxidase [flavin-containing] A	IC 50 (nM)	4.1	N/A	N/A	Details
Pargyline	Amine oxidase [flavin-containing] B	IC 50 (nM)	188	N/A	N/A	Details