ChemistrySelect, vol.8, no.9, 2023 (SCI-Expanded)
Highly effective one-pot synthesis of novel isoindolinones from various 2-benzoylbenzoic acid derivatives with intramolecular cyclization in the presence of chlorosulfonyl isocyanate was reported in mild conditions in the absence a metal catalyst. Novel synthesized compounds were tested against some metabolic enzymes including acetylcholinesterase (AChE), butyrylcholinesterase (BChE), α-glycosidase and carbonic anhydrase I and II (hCA I and hCA II) enzymes that associated with Alzheimer's disease (AD), type-2 diabetes mellitus (T2DM), epilepsy, and glaucoma. A series of novel isoindolinones (2 a–l) were evaluated as highly potent inhibition ability toward AChE (Kis: 2.33–13.81 μM), BChE (Kis: 1.45–12.27 μM), α-glycosidase (Kis: 8.03–23.05 μM), hCA I (Kis: 2.23–17.35 μM) and hCA II (Kis: 2.86–18.13 μM). Also, for these inhibitors, in silico molecular docking simulations and calculations were done with the Autodock Vina program to support the in vitro experimental studies.