Biochemistry Department, College of Medicine, University of Ha'il, Hail, 2440, Saudi Arabia.
Faculty of Biotechnology, October University for Modern Science & Arts (MSA), Giza, Egypt.
Future Med Chem. 2024;16(19):2013-2023. doi: 10.1080/17568919.2024.2393569. Epub 2024 Sep 13.
Current study aims exploration of -benzoxazole bearing -Schiff base scaffolds () as anti-Alzheimer's agents. 2-aminophenol is used as starting materials which react with different reagents in different step to give us -benzoxazole bearing -Schiff base analogs. NMR and HREI-MS techniques were used for characterization. All derivatives demonstrated varied range of activities with IC values 1.10 ± 0.40-24.50 ± 0.90 μM against acetylcholinesterase (AChE) and 1.90 ± 0.70-28.60 ± 0.60 μM against butyrylcholinesterase (BuChE) in contrast to donepezil. In both cases, analog- was found most potent. Molecular docking explored modes of interactions between scaffolds and receptor sites of targeted enzymes. This study offering promising approach for optimization and development of potent inhibitors of cholinesterase enzymes.
本研究旨在探索含苯并恶唑基的席夫碱支架（）作为抗阿尔茨海默病药物。以 2-氨基酚为起始原料，通过不同的试剂在不同的步骤中反应，得到含苯并恶唑基的席夫碱类似物。采用 NMR 和 HREI-MS 技术进行表征。所有衍生物均表现出不同的活性范围，对乙酰胆碱酯酶（AChE）的 IC 值为 1.10±0.40-24.50±0.90 μM，对丁酰胆碱酯酶（BuChE）的 IC 值为 1.90±0.70-28.60±0.60 μM，与多奈哌齐相比。在这两种情况下，类似物-被发现最有效。分子对接探索了支架与靶酶受体结合位点之间的相互作用模式。这项研究为优化和开发胆碱酯酶抑制剂提供了有前途的方法。
