Department of Chemistry, Punjabi University, Patiala 147002, Punjab, India.
Bioorg Med Chem. 2012 Feb 1;20(3):1175-80. doi: 10.1016/j.bmc.2011.12.042. Epub 2011 Dec 30.
Acetylcholinesterase (AChE) enzyme inhibition is an important target for the management of Alzheimer disease (AD) and AChE inhibitors are the main stay drugs for its management. Coumarins are the phytochemicals with wide range of biological activities including AChE inhibition. The scientists have attempted to explore the coumarin template for synthesizing novel AChE inhibitors with additional pharmacological activities including decrease in beta-amyloid (Aβ) deposition and beta-secretase inhibition that are also important for AD management. Most of the designed schemes have involved incorporation of a catalytic site interacting moiety at 3- and 4-positions of the coumarin ring. The present review describes these differently synthesized coumarin derivatives as AChE inhibitors for management of AD.
乙酰胆碱酯酶（AChE）抑制是治疗阿尔茨海默病（AD）的重要靶点，AChE 抑制剂是其治疗的主要药物。香豆素是具有广泛生物活性的植物化学物质，包括 AChE 抑制作用。科学家们试图探索香豆素模板，以合成具有额外药理活性的新型 AChE 抑制剂，包括减少β-淀粉样蛋白（Aβ）沉积和β-分泌酶抑制，这对 AD 管理也很重要。大多数设计方案都涉及在香豆素环的 3-和 4-位引入一个催化部位相互作用的部分。本综述描述了这些不同合成的香豆素衍生物作为 AChE 抑制剂用于 AD 的治疗。
