Novel hybrids of oxoisoaporphine-tryptamine as acetylcholinesterase-induced β-amyloid aggregation inhibitors with improved antioxidant properties
| Autor: | Hai-Tao Zhao, Shu-Ming Zhong, Huang Tang, Jiang-Ke Qin |
|---|---|
| Jazyk: | angličtina |
| Rok vydání: | 2015 |
| Předmět: |
Tryptamine
Antioxidant oxoisoaporphine-tryptamine Oxygen radical absorbance capacity Stereochemistry medicine.drug_class medicine.medical_treatment General Chemistry Acetylcholinesterase In vitro lcsh:Chemistry chemistry.chemical_compound chemistry Biochemistry Acetylcholinesterase inhibitor lcsh:QD1-999 medicine Trolox Binding site Ab antiag-gregating activity Alzheimer’s disease acetylcholinesterase inhibitor |
| Zdroj: | Journal of the Serbian Chemical Society, Vol 80, Iss 2, Pp 127-136 (2015) |
| ISSN: | 1820-7421 0352-5139 |
| Popis: | A series of dual binding site acetylcholinesterase (AChE) inhibitors have been designed, synthesized, and tested for their antioxidant ability and inhibitory potency on AChE and AChE-induced b-amyloid (Ab) aggregation. The new hybrids consist of a unit of 1-azabenzanthrone and a tryptamine or its derivative, connected through a a,w - alkyldiamide bridge. These hybrids exhibit moderate AChE inhibitory activity with IC50 values in the micromolar range and significant in vitro inhibitory activity toward the AChE-induced Ab aggregation. Moreover, six out of the nine hybrids of this series exhibit a higher oxygen radical absorbance capacity than trolox, which makes them promising anti-Alzheimer drug candidates. |
| Databáze: | OpenAIRE |
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