苯并[1,3]二氧杂环戊烯-2(3H)-酮衍生物，单胺氧化酶和胆碱酯酶的多靶点抑制剂：设计、合成与生物活性。
()--Benzyl-1-phenyl-3,4-dihydroisoqunoline-2(1)-carboxamide Derivatives, Multi-Target Inhibitors of Monoamine Oxidase and Cholinesterase: Design, Synthesis, and Biological Activity.
机构信息
College of Nursing, Zhejiang Pharmaceutical University, Ningbo 315153, China.
Food and Pharmacy College, Zhejiang Ocean University, Zhoushan 316022, China.
出版信息
Molecules. 2023 Feb 9;28(4):1654. doi: 10.3390/molecules28041654.
A series of ()-1-phenyl-3,4-dihydroisoquinoline-2(1)-carboxamide derivatives was synthesized and evaluated for inhibitory activity against monoamine oxidase (MAO)-A and-B, acetylcholine esterase (AChE), and butyrylcholine esterase (BChE). Four compounds (, , , and ) showed good inhibitory activity against both MAO-A and MAO-B, and two compounds ( and ) showed selective inhibitory activity against MAO-A, with IC values of 1.38 and 2.48 µM, respectively. None of the compounds showed inhibitory activity against AChE; however, 12 compounds showed inhibitory activity against BChE. None of the active compounds showed cytotoxicity against L929cells. Molecular docking revealed several important interactions between the active analogs and amino acid residues of the protein receptors. This research paves the way for further study aimed at designing MAO and ChE inhibitors for the treatment of depression and neurodegenerative disorders.
合成了一系列（）-1-苯基-3,4-二氢异喹啉-2(1)-甲酰胺衍生物，并评估了它们对单胺氧化酶（MAO）-A 和 -B、乙酰胆碱酯酶（AChE）和丁酰胆碱酯酶（BChE）的抑制活性。四种化合物（、、、）对 MAO-A 和 MAO-B 均显示出良好的抑制活性，两种化合物（和）对 MAO-A 显示出选择性抑制活性，IC 值分别为 1.38 和 2.48 µM。没有一种化合物对 AChE 表现出抑制活性；然而，有 12 种化合物对 BChE 表现出抑制活性。没有活性化合物对 L929 细胞表现出细胞毒性。分子对接揭示了活性类似物与蛋白质受体的氨基酸残基之间的几种重要相互作用。这项研究为进一步研究设计 MAO 和 ChE 抑制剂以治疗抑郁症和神经退行性疾病铺平了道路。
Zotero 插件