Luo Wen, Zhao Yong-Mei, Zhang Zhen, Su Ya-Bin, Wang Chao-Jie
Key Laboratory of Natural Medicine and Immuno-Engineering, Henan University, Kaifeng 475004, China.
Yao Xue Xue Bao. 2012 Jul;47(7):916-21.
A series of tacrine-methoxybenzene hybrids (5a-5i) were designed, synthesized and evaluated as inhibitors of cholinesterases (ChEs). All the compounds had better ChEs inhibitory activities than tacrine with IC50 values at the nanomolar range. Compound 5h exhibited the strongest inhibition on acetylcholinesterase (AChE) with an IC50 value of 6.74 nmol x L(-1) and compound 5f showed the most potent inhibition on butyrylcholinesterase with IC50 value of 3.83 nmol x L(-1). Kinetic and molecular modeling studies showed that these hybrids targeted both the catalytic active site and the peripheral anionic site of AChE.
设计、合成并评估了一系列他克林 - 甲氧基苯杂合物（5a - 5i）作为胆碱酯酶（ChEs）抑制剂。所有化合物的胆碱酯酶抑制活性均优于他克林，其IC50值处于纳摩尔范围。化合物5h对乙酰胆碱酯酶（AChE）表现出最强抑制作用，IC50值为6.74 nmol·L⁻¹，化合物5f对丁酰胆碱酯酶表现出最有效抑制作用，IC50值为3.83 nmol·L⁻¹。动力学和分子模拟研究表明，这些杂合物靶向AChE的催化活性位点和外周阴离子位点。
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