Biological evaluation and docking studies of some benzoxazole derivatives as inhibitors of acetylcholinesterase and butyrylcholinesterase


Temiz-Arpaci O., ARISOY M., SAÇ D., DOĞANÇ F., TAŞCI M. , ŞENOL F. S. , ...Daha Fazla

ZEITSCHRIFT FUR NATURFORSCHUNG SECTION C-A JOURNAL OF BIOSCIENCES, cilt.71, ss.409-413, 2016 (SCI İndekslerine Giren Dergi) identifier identifier identifier

  • Cilt numarası: 71
  • Basım Tarihi: 2016
  • Doi Numarası: 10.1515/znc-2016-0087
  • Dergi Adı: ZEITSCHRIFT FUR NATURFORSCHUNG SECTION C-A JOURNAL OF BIOSCIENCES
  • Sayfa Sayıları: ss.409-413

Özet

A series of 2,5-disubstituted-benzoxazole derivatives (1-13) were evaluated as possible inhibitors of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE). The results demonstrated that the compounds exhibited a broad spectrum of AChE and BChE inhibitory activity ranging between 6.80% and 90.21% except one compound which showed no activity against AChE at the specified molar concentration. Another derivative displayed a similar activity to that of reference drug (galanthamine) for inhibition of AChE and BChE. In addition, molecular docking of the compounds into active site of AChE was performed using recombinant human AChE (PDB ID: 4ey6) in order to understand ligand-protein interactions.