Mahdavi, M. and Hariri, R. and Mirfazli, S.S. and Lotfian, H. and Rastergari, A. and Firuzi, O. and Edraki, N. and Larijani, B. and Akbarzadeh, T. and Saeedi, M. (2019) Synthesis and Biological Activity of Some Benzochromenoquinolinones: Tacrine Analogs as Potent Anti-Alzheimer's Agents. Chemistry and Biodiversity, 16 (4).
Full text not available from this repository.Abstract
Alzheimer's disease (AD) is a well-known neurodegenerative disorder affecting millions of old people worldwide and the corresponding epidemiological data emphasize the importance of the disease. As AD is a multifactorial illness, various single target directed drugs that have reached clinical trials have failed. Therefore, various factors associated with outset of AD have been considered in targeted drug discovery. In this work, various benzochromenoquinolinones were synthesized and evaluated for their cholinesterase and BACE1 inhibitory activities as well as neuroprotective and metal-chelating properties. Among the synthesized compounds, 14-amino-13-(3-nitrophenyl)-2,3,4,13-tetrahydro-1H-benzo6,7chromeno2,3-bquinoline-7,12-dione (6m) depicted the best inhibitory activity toward acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) with IC 50 s of 0.86 and 6.03 μm, respectively. Also, the compound could inhibit β-secretase 1 (BACE1) with IC 50 =19.60 μm and showed metal chelating ability toward Cu 2+ , Fe 2+ , and Zn 2+ . In addition, docking study demonstrated desirable interactions of compound 6m with amino acid residues characterizing AChE, BChE, and BACE1. © 2019 Wiley-VHCA AG, Zurich, Switzerland
| Item Type: | Article |
|---|---|
| Additional Information: | cited By 0 |
| Subjects: | WT Geriatrics. Chronic Disease |
| Depositing User: | eprints admin |
| Date Deposited: | 31 Oct 2020 10:36 |
| Last Modified: | 31 Oct 2020 10:36 |
| URI: | http://eprints.iums.ac.ir/id/eprint/14791 |
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