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


Temiz-Arpaci O., Arisoy M., Sac D., Doganc F., Tasci M., ŞENOL DENİZ F. S. , ...More

ZEITSCHRIFT FUR NATURFORSCHUNG SECTION C-A JOURNAL OF BIOSCIENCES, vol.71, pp.409-413, 2016 (SCI-Expanded) identifier identifier identifier

  • Publication Type: Article / Article
  • Volume: 71
  • Publication Date: 2016
  • Doi Number: 10.1515/znc-2016-0087
  • Journal Name: ZEITSCHRIFT FUR NATURFORSCHUNG SECTION C-A JOURNAL OF BIOSCIENCES
  • Journal Indexes: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Page Numbers: pp.409-413
  • Keywords: acetylcholinesterase, Alzheimer's disease, benzoxazoles, butyrylcholinesterase, enzyme inhibition, TOPOISOMERASE-II INHIBITORS, ANTIMICROBIAL EVALUATION, ALZHEIMERS-DISEASE, ANTICANCER, BENZIMIDAZOLES, ANTIBACTERIAL, ANTIOXIDANT, ANALOGS, BINDING, AGENTS
  • Gazi University Affiliated: Yes

Abstract

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.