SYNTHESIS AND CHOLINESTERASE INHIBITORY ACTIVITIES OF SOME 4-(3/4-NITROPHTHALIMIDO) BENZENESULFONAMIDE DERIVATIVES


Rumanlı H., Uysal Ş. , Soyer Z. , Parlar S. , Alptüzün V.

2nd International Gazi Pharma Symposium Series (GPSS) 2017, Ankara, Türkiye, 11 - 13 Ekim 2017, ss.267

  • Basıldığı Şehir: Ankara
  • Basıldığı Ülke: Türkiye
  • Sayfa Sayıları: ss.267

Özet

Phthalimide is a very important scaffold for medicinal chemists to prepare biologically active molecules [1]. 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 [4], anticonvulsant [5], antihypertensive [6], antibacterial, antiinflammatory, anticancer [7]. 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 [8]. 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