AI Article Synopsis
- New inhibitors of acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) were designed and synthesized, showing potential to block calcium channels and possess antioxidant properties.
- The compound identified as MTDL effectively inhibits AChE and BuChE, demonstrating significant activity with IC50 values of 1.8 μM and 2 μM respectively.
- MTDL also exhibits neuroprotective effects, with notable reductions in oxidative stress damaging agents, making it a promising candidate for further research in Alzheimer's disease treatments.
Article Abstract
We report herein the design, synthesis, biological evaluation, and molecular modelling of new inhibitors of acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE), able to block Ca channels also showing antioxidant and neuroprotective activities. The new MTDL, dialkyl 2,6-dimethyl-4-(4-((5-aminoalkyl)oxy)phenyl)-1,4-dihydropyridine-3,5-dicarboxylate , have been obtained via Hantzsch reaction from appropriate and commercially available precursors. Pertinent biological analysis has prompted us to identify MTDL [dimethyl-4-(4-((5-(4-benzylpiperidin-1-yl)pentyl)oxy)phenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate] as an attractive inhibitor of AChE (1.8 μM) and BuChE (2 μM), Ca channel antagonist (47.72% at 10 μM), and antioxidant (2.54 TE) agent, showing significant neuroprotection 28.68% and 38.29% against HO and O/R, respectively, at 0.3 μM, thus being considered a hit-compound for further investigation in our search for anti-Alzheimer's disease agents.
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| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7589057 | PMC |
| http://dx.doi.org/10.3390/ijms21207652 | DOI Listing |
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