Biological evaluation and in silico study of benzohydrazide derivatives as paraoxonase 1 inhibitors
Özet
Serum paraoxonase 1 (PON1) is found in all mammalian species and is a calcium-dependent hydrolytic enzyme. PON1 hydrolyze several substrates, including carbonates, esters, and organophosphates. In the current study, we aimed to investigate the effect of the presynthesized benzohydrazide derivatives (1-9) on PON1 activity. Benzohydrazide compounds moderate inhibited PON1 with the half-maximal inhibitory concentration values ranging from 76.04 +/- 13.51 to 221.70 +/- 13.59 mu M and K-I values ranging from 38.75 +/- 12.21 to 543.50 +/- 69.76 mu M. Compound 4 (2-amino-4-chlorobenzohydrazide) showed the best inhibition (K-I = 38.75 +/- 12.21 mu M). Molecular docking and ADME-Tox studies of benzohydrazide derivatives were also carried out. In this context, we hope that the results obtained in this study contribute to the determination of the side effects of current and new benzohydrazide-based pharmacological compounds to be developed.
Anahtar kelimeler
Atıf için künye
Korkmaz, I. N., TÜRKEŞ, C., Demir, Y., ÖZTEKİN, A., Özdemir, H., & BEYDEMİR, Ş. (2022). Biological evaluation and in silico study of benzohydrazide derivatives as paraoxonase 1 inhibitors. JOURNAL OF BIOCHEMICAL AND MOLECULAR TOXICOLOGY, 36(11). https://doi.org/10.1002/jbt.23180
BibTeX
@article{korkmaz2022-67315,
author = {Korkmaz, Isil Nihan and TÜRKEŞ, CÜNEYT and Demir, Yeliz and ÖZTEKİN, AYKUT and Özdemir, Hasan and BEYDEMİR, ŞÜKRÜ},
title = {Biological evaluation and in silico study of benzohydrazide derivatives as paraoxonase 1 inhibitors},
journal = {JOURNAL OF BIOCHEMICAL AND MOLECULAR TOXICOLOGY},
year = {2022},
volume = {36},
number = {11},
issn = {1095-6670},
doi = {10.1002/jbt.23180},
url = {https://akademik.atauni.edu.tr/yayinlar/67315-biological-evaluation-and-in-silico-study-of-benzohydrazide-derivatives-as}
}