Synthesis, characterization, and molecular docking analysis of novel benzimidazole derivatives as cholinesterase inhibitors.
作者： Yeong Keng Yoon , Mohamed Ashraf Ali , Ang Chee Wei , Tan Soo Choon , Kooi-Yeong Khaw
DOI: 10.1016/J.BIOORG.2013.06.008
关键词:
摘要: Two series of novel acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitors containing benzimidazole core structure were synthesized by a four-step reaction pathway starting from 4-fluoro-3-nitrobenzoic acid as the basic compound. The benzimidazoles was characterized confirmed elemental mass spectral analyses well (1)H NMR spectroscopic data. Of 34 compounds, three revealed AChE inhibition with IC50<10 μM. highest inhibitory activity (IC50=5.12 μM for IC50=8.63 BChE) corresponds to compound 5IIc (ethyl 1-(3-(1H-imidazol-1-yl)propyl)-2-(4-nitrophenyl)-1H-benzo[d]imidazole-5-carboxylate). relationship between lipophilicity chemical structures their limited structure-activity discussed.
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