Synthesis of Spiro-oxindole Analogs Engrafted Pyrazole Scaffold as Potential Alzheimer's Disease Therapeutics: Anti-oxidant, Enzyme Inhibitory and Molecular Docking Approaches

About 19 spirooxindole analogs 8 a-s engrafted with pyrazole scaffolds were designed and constructed via [3+2] cycloaddition reaction (32CA) approach. The synthesized spirooxindole analogs was screened for anti-cholinesterase against acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) and antioxidant potentials against DPPH. The compounds 8 h and 8 i showed the strongest acetylcholine esterase (AChE) and butyrylcholinesterase (BChE) inhibition with IC50 values of 30 mu g/mL respectively. The highest anti-oxidant potential was demonstrated by compounds 8 p with IC50 values of 240 mu g/mL, respectively. Molecular docking was used to study their interaction with the active site of enzymes.

Automated summary

A series of 19 spirooxindole analogs grafted with pyrazole scaffolds were synthesized using the [3+2] cycloaddition reaction approach. The synthesized compounds were evaluated for their anti-cholinesterase and antioxidant activities. Compounds 8 h and 8 i showed the strongest inhibition against acetylcholinesterase and butyrylcholinesterase, while compound 8 p exhibited the highest antioxidant potential. Molecular docking studies were conducted to investigate the interaction between the compounds and the active site of enzymes.