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首页> 外文期刊>Chemical biology and drug design >Novel Potent and Selective Acetylcholinesterase Inhibitors as Potential Drugs for the Treatment of Alzheimer's Disease: Synthesis, Pharmacological Evaluation, and Molecular Modeling of Amino-Alkyl-Substituted Fluoro-Chalcones Derivatives
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Novel Potent and Selective Acetylcholinesterase Inhibitors as Potential Drugs for the Treatment of Alzheimer's Disease: Synthesis, Pharmacological Evaluation, and Molecular Modeling of Amino-Alkyl-Substituted Fluoro-Chalcones Derivatives

机译：新型有效和选择性乙酰胆碱酯酶抑制剂作为治疗阿尔茨海默氏病的潜在药物：氨基烷基取代的氟代-卤代衍生物的合成，药理学评估和分子模型

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摘要

A new series of-fluoro chalcones-substituted amino-alkyl derivatives (3a3l) were designed, synthesized, characterized and evaluated for the inhibitory activity against acetylcholinesterase and butyrylcholinesterase. The results showed that the alteration of fluorine atom position and amino-alkyl groups markedly influenced the activity and the selectivity of chalcone derivates in inhibiting acetylcholinesterase and butyrylcholinesterase. Among them, compound 3l possesses the most potent inhibitory against acetylcholinesterase (IC50=0.21 +/- 0.03mol/L), and the highest selectivity for acetylcholinesterase over butyrylcholinesterase (IC50 (BuChE)/IC50 (AChE)=65.0). Molecular modeling and enzyme kinetic study on compound 3l supported its dual acetylcholinesterase inhibitory profile, simultaneously binding at the catalytic active and peripheral anionic site of the enzyme.
机译：设计，合成，表征并评估了一系列新的氟代查耳酮取代的氨基烷基衍生物（3a31）对乙酰胆碱酯酶和丁酰胆碱酯酶的抑制活性。结果表明，氟原子位置和氨基烷基的变化显着影响查尔酮衍生物抑制乙酰胆碱酯酶和丁酰胆碱酯酶的活性和选择性。其中，化合物3l对乙酰胆碱酯酶的抑制作用最强（IC50 = 0.21 +/- 0.03mol / L），对乙酰胆碱酯酶的选择性高于对丁酰胆碱酯酶的选择性（IC50（BuChE）/ IC50（AChE）= 65.0）。化合物3l的分子建模和酶动力学研究支持其双重乙酰胆碱酯酶抑制特性，同时在酶的催化活性和外围阴离子位点结合。

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