Article
2022
·
10 citations
Synthesis and aldose reductase inhibition effects of celecoxib derivatives containing pyrazole linked-sulfonamide moiety
Abstract
In this article, we report the synthesis of Celecoxib derivatives containing the pyrazole-linked sulfonamide moiety. The enzyme inhibition effects of these derivatives on aldose reductase (AR) were also investigated. The IC50 values of the pyrazole sulfonamide derivatives were determined to be in the range of 40.76-8.25 mu M. Among the synthesized derivatives, the compound 16 showed the strongest inhibition effect against the AR enzyme, with an IC50 value of 8.25 mu M. Molecular docking studies were carried out to determine the interactions of the synthesized compounds with the AR enzyme, and ADMET studies were performed to assess the pharmacokinetic and drug-likeness properties.
Keywords
Pyrazole
Sulfonamide
Aldose reductase
Molecular docking
ADMET
ONE-POT SYNTHESIS
BIOLOGICAL EVALUATION
DOCKING
ANALOGS
PROTEIN
WoS Categories
Biochemistry & Molecular Biology
Chemistry, Organic
Sustainable Development Goals
Citation
- Journal
- BIOORGANIC CHEMISTRY
- Year
- 2022
- Volume
- 128
- ISSN
- 0045-2068
- eISSN
- 1090-2120
- DOI
- 10.1016/j.bioorg.2022.106086
- WoS UID
- WOS:000848488400003