Design, Synthesis and Acetylcholinesterase and Butylcholinesterase Inhibi-tion Activity of Novel 1-(Alkyl)-3-(2-oxo-2H-chromenyloxy Acetamido) methylpyridinium Salts

被引:0
作者
Fard, Mehri Abdollahi [1 ]
Manafi, Mohammadreza [1 ]
Motevalian, Manijeh [2 ,3 ]
Homami, Seyed Saied [1 ]
机构
[1] Islamic Azad Univ, Fac Sci, Dept Appl Chem, South Tehran Branch, Tehran, Iran
[2] Iran Univ Med Sci, Med Sch, Tehran, Iran
[3] Iran Univ Med Sci, Razi Drug Res Ctr, Tehran, Iran
关键词
Coumarin; synthesis; Alzheimer's disease; enzyme inhibition; AChE inhibition; BuChe inhibition; TACRINE-COUMARIN HYBRIDS; ALZHEIMERS-DISEASE; CHOLINESTERASE; DERIVATIVES; DISCOVERY; DRUGS;
D O I
10.2174/1570178617999200818165935
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
In this paper, a novel series of 1-(alkyl)-3-(2-oxo-2H-chromenyloxy acetamido) methylpyridinium salts were synthesized in a simple and efficient way. The method showed to be facile and the compounds were obtained in high isolated yields. All the synthesized compounds were characterized by 1H NMR, 13C NMR, FT-IR, Mass and elemental analysis. AChE and BuChE inhibition activity of the synthesized compounds were evaluated and the results showed that all the compounds were active in the inhibition of the mentioned enzymes. All the compounds were active in the inhibition of the two studied enzymes. Among all the compounds, the compound 6a (1.85 mu M) and 6i (0.106 mu M) showed the highest inhibition activity against AChE and BuChE, respectively. The kinetic study was performed to get more insight into the mechanism of action of the synthesized compounds. Docking studies were also performed to obtain the interactions between the synthesized compounds and the enzymes.
引用
收藏
页码:538 / 546
页数:9
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