2nd International Gazi Pharma Symposium Series (GPSS) 2017, Ankara, Türkiye, 11 - 13 Ekim 2017, ss.267
Phthalimide is a very important scaffold for medicinal chemists to prepare biologically active
molecules . To date, several phthalimide derivatives with various bioactivities such as
anticancer, anti-inflammatory, anticonvulsant and acetylcholinesterase (AChE) inhibitory
activity have been synthesized [2, 3]. On the other hand, sulfonamide derivatives are
another important class of pharmacophores constituting various pharmacological acitivities
such as diuretic , anticonvulsant , antihypertensive , antibacterial, antiinflammatory, anticancer . In the present study, we synthesized four 4-(3/4-
nitrophthalimido)benzenesulfonamide derivatives bearing two pharmacophore groups
(phthalimide and sulfonamide) and evaluated their cholinesterase inhibitory activities
(Figure 1). Structure of the synthesized compounds were confirmed by spectral analyses.
The cholinesterase inhibitory activities of the title compounds were evaluated by modified
Ellman’s method with rivastigmine as the reference compound . It was observed that all
compounds exhibited higher inhibitory activity against AChE. In addition, the compounds
showed better AChE inhibition when compared with the reference compound rivastigmine.
Compound 3 appeared as the most potent derivative against AChE with IC50=2.22±0.05 µM
in the tested compounds