Synthesis of 2‐(2‐oxo‐2 H ‐chromen‐4‐yl)acetamides as potent acetylcholinesterase inhibitors and molecular insights into binding interactions

• Main Authors: Kara, Jiraporn, Suwanhom, Paptawan, Wattanapiromsakul, Chatchai, Nualnoi, Teerapat, Puripattanavong, Jindaporn, Khongkow, Pasarat, Lee, Vannajan Sanghiran, Gaurav, Anand, Lomlim, Luelak
• Format: Article
• Published: Wiley-VCH Verlag 2019
• Subjects: Q Science (General); QD Chemistry
• Online Access: http://eprints.um.edu.my/24187/; https://doi.org/10.1002/ardp.201800310

Sixteen novel coumarin-based compounds are reported as potent acetylcholinesterase (AChE) inhibitors. The most active compound in this series, 5a (IC50 0.04 ± 0.01 µM), noncompetitively inhibited AChE with a higher potency than tacrine and galantamine. Compounds 5d, 5j, and 5 m showed a moderate ant...