Synthesis, characterization, molecular docking and biological activities of novel pyrazoline derivatives
Özet
In this study, synthesis of ethyl 2-((4-bromophenyl)diazenyl)-3-oxo-phenylpropanoate 1 was carried out and a series of new 3H-pyrazol-3-ones (P1-7) were synthesized from 1 as well as various hydrazines. The obtained yields of the synthesized compounds were moderate (40-70%) and these compounds were confirmed by spectral data. These novel pyrazoline derivatives were effective inhibitor compounds of the human carbonic anhydrase I and II isozymes (hCAs I and II) and of the acetylcholinesterase (AChE) enzyme, with K-i values in the range of 17.4-40.7 nM for hCA I, 16.1-55.2 nM for hCA II, and 48.2-84.1 nM for AChE. In silico studies were performed on the compounds inhibiting hCA I, hCA II, and AChE receptors. On the basis of the findings, the inhibition profile of the new pyrazoline compounds at the receptors was determined.
Anahtar kelimeler
Atıf için künye
Turkan, F., Cetin, A., Taslimi, P., KARAMAN, H., & Gülçin, İ. (2019). Synthesis, characterization, molecular docking and biological activities of novel pyrazoline derivatives. Archiv der Pharmazie, 352(6). https://doi.org/10.1002/ardp.201800359
BibTeX
@article{turkan2019-67680,
author = {Turkan, Fikret and Cetin, Adnan and Taslimi, Parham and KARAMAN, Hasan and Gülçin, İlhami},
title = {Synthesis, characterization, molecular docking and biological activities of novel pyrazoline derivatives},
journal = {Archiv der Pharmazie},
year = {2019},
volume = {352},
number = {6},
issn = {0365-6233},
doi = {10.1002/ardp.201800359},
url = {https://akademik.atauni.edu.tr/yayinlar/67680-synthesis-characterization-molecular-docking-and-biological-activities-of-novel}
}