Microwave-Assisted Synthesis, Molecular Docking, and Cholinesterase Inhibitory Activities of New Ethanediamide and 2-Butenediamide Analogues
Özet
A novel series of meta-substituted ethanediamide and 2-butenediamide derivatives were synthesized and tested for their ability to inhibit electric eel acetylcholinesterase (AChE) and equine serum butyrylcholinesterase (BuChE). The synthesized compounds were evaluated against ChE enzymes using the colorimetric method described by Ellman et al. (Biochem. Pharmacol., 7, 1961). It was revealed that some synthesized compounds exhibited high anticholinesterase activity, among which compounds if and 2f were the most active inhibitors against BuChE (IC50 value=1.471 mu M) and AChE (IC50 value=2.099 mu M), respectively. Docking simulations revealed that the inhibitors if and 2f are capable of simultaneously binding the peripheral anionic site as well as the catalytic anionic site of both ChE enzymes. These derivatives are considered interesting candidates for Alzheimer's disease treatment.
Anahtar kelimeler
Atıf için künye
Koca, M., Yerdelen, K. Ö., Anıl, B., & KASAP, Z. (2015). Microwave-Assisted Synthesis, Molecular Docking, and Cholinesterase Inhibitory Activities of New Ethanediamide and 2-Butenediamide Analogues. CHEMICAL & PHARMACEUTICAL BULLETIN, 63(3), 210–217. https://doi.org/10.1248/cpb.c14-00754
BibTeX
@article{koca2015-19766,
author = {Koca, Mehmet and Yerdelen, Kadir Özden and Anıl, Barış and KASAP, Zeynep},
title = {Microwave-Assisted Synthesis, Molecular Docking, and Cholinesterase Inhibitory Activities of New Ethanediamide and 2-Butenediamide Analogues},
journal = {CHEMICAL & PHARMACEUTICAL BULLETIN},
year = {2015},
volume = {63},
number = {3},
pages = {210--217},
issn = {0009-2363},
doi = {10.1248/cpb.c14-00754},
url = {https://akademik.atauni.edu.tr/yayinlar/19766-microwave-assisted-synthesis-molecular-docking-and-cholinesterase-inhibitory}
}