期刊
JOURNAL OF MOLECULAR STRUCTURE
卷 1155, 期 -, 页码 797-806出版社
ELSEVIER SCIENCE BV
DOI: 10.1016/j.molstruc.2017.11.079
关键词
N-heterocyclic carbenes; Carbonic anhydrase; Cholinesterase; alpha-Glycosidase; X-ray diffraction
资金
- Dokuz Eylul University [2010.KB.FEN.13]
- Inonu University Research Fund [I.U.B.A.P.2016/125]
This study contains novel a serie synthesis of N-heterocyclic carbene (NHC) precursors that 2-hydroxyethyl substituted. The NHC precursors have been prepared from 1-(2-hydroxyethyl)benzimidazole and alkyl halides. The novel NHC precursors have been characterized by using H-1 NMR, C-13 NMR, FTIR spectroscopy and elemental analysis techniques. Molecular and crystal structures of 2a, 2d, 2e, 2f and 2g were obtained with single-crystal X-ray diffraction studies. These novel NHC precursor's derivatives effectively inhibited the a-glycosidase, cytosolic carbonic anhydrase I and II isoforms (hCA I and II), butyrylcholinesterase (BChE) and acetylcholinesterase (AChE). Inhibition constant (K-i) were found in the range of 0.30-9.22 nM for alpha-glycosidase, 13.90-41.46 nM for hCA I, 12.82-49.95 nM for hCA II, 145.82-882.01 nM for BChE, and 280.92-1370.01 nM for AChE, respectively. (C) 2017 Elsevier B.V. All rights reserved.
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