Design, synthesis, and evaluation of indanone derivatives as acetylcholinesterase inhibitors and metal-chelating agents
| Autor: | Fangfei Qin, Wenjun Shan, Ling Huang, Fanchao Meng, Xingshu Li, Fei Mao |
|---|---|
| Rok vydání: | 2012 |
| Předmět: |
Pyridines
Aché Stereochemistry Clinical Biochemistry Pharmaceutical Science Inhibitory postsynaptic potential Biochemistry Structure-Activity Relationship chemistry.chemical_compound Alzheimer Disease Drug Discovery medicine Humans Donepezil Molecular Biology IC50 Chelating Agents Organic Chemistry Acetylcholinesterase language.human_language Kinetics chemistry Design synthesis Metals Drug Design Indans Metal Chelating Agents language Molecular Medicine Cholinesterase Inhibitors Piperidine medicine.drug |
| Zdroj: | Bioorganic & Medicinal Chemistry Letters. 22:4462-4466 |
| ISSN: | 0960-894X |
| Popis: | A series of novel indanone derivatives was designed, synthesised and evaluated as potential agents for Alzheimer’s disease. Among them, compound 6a, with a piperidine group linked to indone by a two-carbon spacer, exhibited the most potent inhibitor activity, with an IC50 of 0.0018 μM for AChE; the inhibitory activity of this compound was 14-fold more potent than that of donepezil. Furthermore, these compounds also exhibited good metal-chelating ability. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
|
Full Text from ScienceDirect