New Advances in Chemical Research, May 2021. The prevalence of solvent effects in heterogeneous catalysis in condensed media has motivated developing quantitative kinetic, and theoretical assessments of solvent structures and transition states. Recommanded Product: Methyl 4-bromobenzo[b]thiophene-2-carboxylate, C10H7BrO2S. A document type is Article, introducing its new discovery., Recommanded Product: Methyl 4-bromobenzo[b]thiophene-2-carboxylate
Cholinesterase inhibitor plays an important role in the treatment of patients with Alzheimer?s disease (AD). Herein, we report the medicinal chemistry efforts leading to a new series of 1,3-dimethylbenzimidazolinone derivatives. Among the synthesised compounds, 15b and 15j showed submicromolar IC50 values (15b, eeAChE IC50 = 0.39 ± 0.11 muM; 15j, eqBChE IC50 = 0.16 ± 0.04 muM) towards acetylcholinesterase (AChE) and butyrylcholinesterase (BChE). Kinetic and molecular modelling studies revealed that 15b and 15j act in a competitive manner. 15b and 15j showed neuroprotective effect against H2O2-induced oxidative damage on PC12 cells. This effect was further supported by their antioxidant activity determined in a DPPH assay in vitro. Morris water maze test confirmed the memory amelioration effect of the two compounds in a scopolamine-induced mouse model. Moreover, the hepatotoxicity of 15b and 15j was lower than tacrine. In summary, these data suggest 15b and 15j are promising multifunctional agents against AD.
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Reference：
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem