| Title : Synthesis, characterization, and molecular docking analysis of novel benzimidazole derivatives as cholinesterase inhibitors - Yoon_2013_Bioorg.Chem_49C_33 |
| Author(s) : Yoon YK , Ali MA , Wei AC , Choon TS , Khaw KY , Murugaiyah V , Osman H , Masand VH |
| Ref : Bioorg Chem , 49C :33 , 2013 |
|
Abstract :
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 structure of the novel benzimidazoles was characterized and confirmed by the elemental and mass spectral analyses as well as 1H NMR spectroscopic data. Of the 34 novel synthesized compounds, three benzimidazoles revealed AChE inhibition with IC50<10muM. The highest inhibitory activity (IC50=5.12muM for AChE and IC50=8.63muM for BChE) corresponds to the compound 5IIc (ethyl 1-(3-(1H-imidazol-1-yl)propyl)-2-(4-nitrophenyl)-1H-benzo[d]imidazole-5-carboxyla te). The relationship between lipophilicity and the chemical structures as well as their limited structure-activity relationship was discussed. |
| PubMedSearch : Yoon_2013_Bioorg.Chem_49C_33 |
| PubMedID: 23886696 |
Yoon YK, Ali MA, Wei AC, Choon TS, Khaw KY, Murugaiyah V, Osman H, Masand VH (2013)
Synthesis, characterization, and molecular docking analysis of novel benzimidazole derivatives as cholinesterase inhibitors
Bioorg Chem
49C :33
Yoon YK, Ali MA, Wei AC, Choon TS, Khaw KY, Murugaiyah V, Osman H, Masand VH (2013)
Bioorg Chem
49C :33