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

Yerdelen, Kadir Özden; Koca, Mehmet; Anıl, Barış; SEVINDIK, Handan Gökben; KASAP, Zeynep; Halıcı, Zekai; TURKAYDIN, Kubra; GUNESACAR, Gulsen

doi:10.1016/j.bmcl.2015.10.051

Makale Tam Makale Uluslararası 2015

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

Kadir Özden Yerdelen, Mehmet Koca, Barış Anıl, Handan Gökben SEVINDIK, Zeynep KASAP, Zekai Halıcı, Kubra TURKAYDIN, Gulsen GUNESACAR

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS Cilt 25 · Sayı 23 · ss. 5576–5582 · 01.12.2015

DOI ile aç

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.

Anahtar kelimeler

INHIBITORS AChE BuChE Acetylcholinesterase Butyrylcholinesterase 2-butenediamide Alzheimer AMYLOID-BETA ANTICHOLINESTERASE ACTIVITY DOCKING ANALOGS AGGREGATION Donepezil

Atıf için künye

Yerdelen, K. Ö., Koca, M., Anıl, B., SEVINDIK, H. G., KASAP, Z., Halıcı, Z., TURKAYDIN, K., & GUNESACAR, G. (2015). Synthesis of donepezil-based multifunctional agents for the treatment of Alzheimer's disease. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 25(23), 5576–5582. https://doi.org/10.1016/j.bmcl.2015.10.051

BibTeX

@article{yerdelen2015-19762,
  author = {Yerdelen, Kadir Özden and Koca, Mehmet and Anıl, Barış and SEVINDIK, Handan Gökben and KASAP, Zeynep and Halıcı, Zekai and TURKAYDIN, Kubra and GUNESACAR, Gulsen},
  title = {Synthesis of donepezil-based multifunctional agents for the treatment of Alzheimer's disease},
  journal = {BIOORGANIC & MEDICINAL CHEMISTRY LETTERS},
  year = {2015},
  volume = {25},
  number = {23},
  pages = {5576--5582},
  issn = {0960-894X},
  doi = {10.1016/j.bmcl.2015.10.051},
  url = {https://akademik.atauni.edu.tr/yayinlar/19762-synthesis-of-donepezil-based-multifunctional-agents-for-the-treatment-of}
}