scholarly journals Multitarget Strategy to Address Alzheimer's Disease: Design, Synthesis, Biological Evaluation, and Computational Studies of Coumarin-Based Derivatives

ChemMedChem ◽  
2015 ◽  
Vol 11 (12) ◽  
pp. 1296-1308 ◽  
Author(s):  
Serena Montanari ◽  
Manuela Bartolini ◽  
Paolo Neviani ◽  
Federica Belluti ◽  
Silvia Gobbi ◽  
...  
Keyword(s):  
Alzheimer’S Disease ◽  
Alzheimer's Disease ◽  
Biological Evaluation ◽  
Computational Studies ◽  
Design Synthesis

scholarly journals Synthesis of Hantzsch Adducts as Cholinesterases and Calcium Flux inhibitors, Antioxidants and Neuroprotectives

2020 ◽  
Vol 21 (20) ◽  
pp. 7652
Author(s):  
Irene Pachón Angona ◽  
Helene Martin ◽  
Solene Daniel ◽  
Ignacio Moraleda ◽  
Alexandre Bonet ◽  
...  
Keyword(s):  
Alzheimer’S Disease ◽  
Alzheimer's Disease ◽  
Molecular Modelling ◽  
Biological Evaluation ◽  
Calcium Flux ◽  
Hantzsch Reaction ◽  
Design Synthesis ◽  
Biological Analysis

We report herein the design, synthesis, biological evaluation, and molecular modelling of new inhibitors of acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE), able to block Ca+2 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 3a-p, have been obtained via Hantzsch reaction from appropriate and commercially available precursors. Pertinent biological analysis has prompted us to identify MTDL 3h [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+2 channel antagonist (47.72% at 10 μM), and antioxidant (2.54 TE) agent, showing significant neuroprotection 28.68% and 38.29% against H2O2, 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.

Sign in / Sign up

Export Citation Format

Share Document