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

Abstract

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 μg/mL respectively. The highest anti-oxidant potential was demonstrated by compounds 8 p with IC50 values of 240 μg/mL, respectively. Molecular docking was used to study their interaction with the active site of enzymes.