Anticholinesterase activity screening of some novel dithiocarbamate derivatives including piperidine and piperazine moieties

LEVENT S., ACAR ÇEVİK U., SAĞLIK B. N., ÖZKAY Y., CAN Ö. D., DEMİR ÖZKAY Ü., ...Daha Fazla

PHOSPHORUS SULFUR AND SILICON AND THE RELATED ELEMENTS, cilt.192, sa.4, ss.469-474, 2017 (SCI-Expanded) identifier identifier

  • Yayın Türü: Makale / Tam Makale
  • Cilt numarası: 192 Sayı: 4
  • Basım Tarihi: 2017
  • Doi Numarası: 10.1080/10426507.2016.1259228
  • Dergi Adı: PHOSPHORUS SULFUR AND SILICON AND THE RELATED ELEMENTS
  • Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus, Index Chemicus (IC)
  • Sayfa Sayıları: ss.469-474
  • Anahtar Kelimeler: Alzheimer's disease, dithiocarbamate, piperazine, piperidine, AChE, BChE, BIOLOGICAL EVALUATION, ALZHEIMERS-DISEASE, ACETYLCHOLINESTERASE INHIBITORS, CHOLINESTERASE-INHIBITORS, N-BENZYLPIPERIDINE, IN-SILICO, ANTIACETYLCHOLINESTERASE ACTIVITY, MOLECULAR DOCKING, DESIGN, BEARING
  • Anadolu Üniversitesi Adresli: Evet

Özet

The present study was undertaken to synthesize some novel lipophilic piperazine and piperidinedithiocarbamates and investigate their inhibitory potencies against cholinesterase enzymes. In the synthetic studies, 44 new compounds were isolated. The structures of the synthesized compounds were confirmed by spectroscopic analyses. Enzymatic studies were carried out using modified Ellman's assay against Acetyl cholinesterase (AChE) and Butrylcholinesterase (BChE) enzymes, and it was observed that some of the compounds selectively inhibit AChE. Theoretical ADME predictions were calculated for selected compounds in the series. Enzyme kinetics and molecular docking studies were performed for the most active compound C41 and nature of inhibition and interactions between enzyme and ligand were explained.