Synthesis of donepezil-based multifunctional agents for the treatment of Alzheimer's disease

Yerdelen K. Ö., KOCA M., ANIL B., SEVINDIK H. G., KASAP Z., HALICI Z., ...Daha Fazla

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, cilt.25, sa.23, ss.5576-5582, 2015 (SCI-Expanded) identifier identifier identifier

  • Yayın Türü: Makale / Tam Makale
  • Cilt numarası: 25 Sayı: 23
  • Basım Tarihi: 2015
  • Doi Numarası: 10.1016/j.bmcl.2015.10.051
  • Dergi Adı: BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
  • Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Sayfa Sayıları: ss.5576-5582
  • Anahtar Kelimeler: Donepezil, Amyloid beta, Alzheimer, AChE, BuChE, AMYLOID-BETA, ANTICHOLINESTERASE ACTIVITY, ACETYLCHOLINESTERASE, INHIBITORS, DOCKING, AGGREGATION, ANALOGS, ACHE, BUTYRYLCHOLINESTERASE, 2-BUTENEDIAMIDE
  • Atatürk Üniversitesi Adresli: Evet

Özet

Amyloid beta (A beta) and cholinesterase enzymes (AChE, BuChE) are important biological targets for the effective treatment of Alzheimer's disease. In this study, the aim was to synthesize new donepezil-like secondary amide compounds that display a potent inhibition of cholinesterases and A beta with antioxidant and metal chelation abilities. All test compounds showed activities against both ChEs and beta(1-42) inhibition. The most encouraging compound, 20, is an AChE inhibitor with high anti-aggregation activity (55.3%). Based on the results, compound 20 may be a promising structure in further research for new anti-Alzheimer's agents. (C) 2015 Elsevier Ltd. All rights reserved.