Synthesis and molecular docking studies of some 4-phthalimidobenzenesulfonamide derivatives as acetylcholinesterase and butyrylcholinesterase inhibitors
Makaleler > Tam Makale · 2016
Yazarlar: Zeynep SOYER, Şirin UYSAL OL, Sülünay PARLAR ÇOŞKUN, Ayşe Hande TARİKOĞULLARI DOĞAN, Vildan ALPTÜZÜN
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, SCI Expanded İndekslerine Giren Dergi, Uluslararası, 2016, cilt 32, ss 13-19
DOI: 10.1080/14756366.2016.1226298
Özet
A series of 4-phthalimidobenzenesulfonamide derivatives were designed, synthesized and evaluated for the inhibitory activities against acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE). Structures of the title compounds were confirmed by spectral and elemental analyses. The cholinesterase (ChE) inhibitory activity studies were carried out using Ellman's colorimetric method. The biological activity results revealed that all of the title compounds (except for compound 8) displayed high selectivity against AChE. Among the tested compounds, compound 7 was found to be the most potent against AChE (IC50 = 1.35 +/- 0.08 mu M), while compound 3 exhibited the highest inhibition against BuChE (IC50 = 13.41 +/- 0.62 mu M). Molecular docking studies of the most active compound 7 in AChE showed that this compound can interact with both the catalytic active site (CAS) and the peripheral anionic site (PAS) of AChE.