Srour_2018_Bioorg.Chem_83_226

In this work, we describe the regioselective synthesis of some new dispiro[indene-2,3'-pyrrolidine-2',3''-indoline]-1,2''(3H)-dione 4-29 attributable to the previously described methods. All the new chemical entities were assessed in-vitro as inhibitors of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) enzymes; while no significant inhibitory activity for the tested compounds were assigned on AChE, compounds 4, 27, 29, 28 and 15 were the most active against BChE enzyme with IC50=13.7microM, 21.8microM, 22.1microM, 22.9microM and 24.9microM respectively compared to Donepezil (IC50=0.72microM). Compound 4 was found to have a mixed type mode of inhibition, the bioactivity of the new chemical entities (N=26, n=5, R(2)=0.893, R(2) cvOO=0.831, R(2) cvMO=0.838, F=33.32, s(2)=0.003) was elucidated via a statistically significant QSAR model utilizing CODESSA-Pro software that validated the observed results.