| Literature DB >> 23988412 |
Mehdi Khoobi1, Masoumeh Alipour, Alireza Moradi, Amirhossein Sakhteman, Hamid Nadri, Seyyede Faeze Razavi, Mehdi Ghandi, Alireza Foroumadi, Abbas Shafiee.
Abstract
Novel hybrid derivatives of two known scaffolds; tetrahydroaminoquinoline and coumarin were synthesized and evaluated for both acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) activities. By means of an efficient nanocatalyst, the reaction time for the syntheses of the target compounds was reduced. Subsequently, Ellman's modified method was used to evaluate the enzyme inhibitory activity of the synthesized structures. It was observed that most hybrid structures were moderate to potent inhibitors of AChE compared to Tacrine as the reference drug among which 7f with 4-fluorophenyl substituent was the most active compound (IC50=5 nM).Entities:
Keywords: Alzheimer's disease; Cholinesterase inhibitor; Coumarin; Docking study; Tacrine
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Year: 2013 PMID: 23988412 DOI: 10.1016/j.ejmech.2013.07.045
Source DB: PubMed Journal: Eur J Med Chem ISSN: 0223-5234 Impact factor: 6.514