Synthesis and aldose reductase inhibition effects of celecoxib derivatives containing pyrazole linked-sulfonamide moiety

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.

Dergi

BIOORGANIC CHEMISTRY

Yıl

2022

Cilt

128

ISSN

0045-2068

eISSN

1090-2120

DOI

10.1016/j.bioorg.2022.106086

WoS UID

WOS:000848488400003