Sheng Rong, Lin Xiao, Li Jing-ya, Hu Yong-zhou
ZJU-ENS Joint Laboratory of Medicinal Chemistry, School of Pharmaceutical Science, Zhejiang University, Hangzhou 310031, China.
Yao Xue Xue Bao. 2006 Feb;41(2):115-20.
To design and synthesize novel AchE inhibitors.
The condensation of 2-bromo-5, 6-dimethoxy-indan-1-one with various aminoalkyl phenols in the presence of K2CO3 and acetonitrile gave the corresponding title compounds, and the in vitro AchE and BchE inhibitory activities were evaluated by the modified Ellman method.
Sixteen novel target compounds 8a - p were synthesized, their structures were confirmed by 1H NMR, MS, IR and elemental analysis. Preliminary pharmacological test demonstrated that most of these compounds displayed high AchE inhibitory activities, the IC50 of the most potent inhibitor 8h was 50.0 nmol x L(-1), similar to that of Huperzine A (IC50 = 53.0 nmol x L(-1)), while all the compounds were almost inactive against BchE.
2-Phenoxy-indan-1-one derivatives exhibit high activities of AchE inhibition and are worthy of further investigation.
设计并合成新型乙酰胆碱酯酶（AchE）抑制剂。
在碳酸钾和乙腈存在的条件下，2-溴-5,6-二甲氧基茚满-1-酮与各种氨基烷基酚缩合得到相应的目标化合物，并采用改良的Ellman法评估其体外AchE和丁酰胆碱酯酶（BchE）抑制活性。
合成了16种新型目标化合物8a - p，其结构经1H NMR、质谱（MS）、红外光谱（IR）和元素分析确证。初步药理试验表明，这些化合物大多表现出较高的AchE抑制活性，最有效抑制剂8h的半数抑制浓度（IC50）为50.0 nmol·L-1，与石杉碱甲（IC50 = 53.0 nmol·L-1）相似，而所有化合物对BchE几乎无活性。
2-苯氧基茚满-1-酮衍生物表现出较高的AchE抑制活性，值得进一步研究。
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