期刊
JOURNAL OF MOLECULAR STRUCTURE
卷 1170, 期 -, 页码 160-169出版社
ELSEVIER SCIENCE BV
DOI: 10.1016/j.molstruc.2018.05.077
关键词
N-heterocyclic carbenes precursors; Benzimidazole; Single-crystal X-ray diffraction; Carbonic anhydrase; Acetylcholinesterase; Enzyme inhibition
资金
- Dokuz Eylul University [2010.KB.FEN.13]
This paper reports the synthesis of 2-(4-hydroxyphenyl)ethyl and 2-(4-nitrophenyl)ethyl substituted benzimidazolium salts. The benzimidazolium salts were synthesized by N-substituted benzimidazolium and aryl halides. The 2-(4-hydroxyphenyl)ethyl and 2-(4-nitrophenyl)ethyl substituted benzimidazolium salts were characterized by using H-1 NMR, C-13 NMR, FT-IR spectroscopy and elemental analysis techniques. Molecular and crystal structure of the complex 2d and 3d were obtained by single-crystal X-ray diffraction method. Additionally, The enzyme inhibition activities of the benzimidazolium salts were investigated. These 2-(4-hydroxyphenyl)ethyl and 2-(4-nitrophenyl)ethyl substituted benzimidazolium salts (1, 2a-g, and 3a-f) showed good inhibitory action against acetylcholinesterase (AChE), and human (h) carbonic anhydrase (CA) isoforms I, and II. Ki values for AChE were in range of 5.97 +/- 0.56 -23.15 +/- 3.98 nM. On the other hand, the hCA I, and II isoenzymes were effectively inhibited by these compounds, with K-i values in the range of 17.33 +/- 4.55-99.23 +/- 44.91 nM for hCA I, and 33.98 +/- 3.43 -113.23 +/- 39.31 nM for hCA II, respectively. (C) 2018 Elsevier B.V. All rights reserved.
作者
我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。
推荐
暂无数据