Journal
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 146, Issue -, Pages 577-587Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2018.01.054
Keywords
Anti-inflammatory; COX-2 inhibitors; COX-1/COX-2 inhibition; Cyclocoumarol; Cyclooxygenase; Docking study
Categories
Funding
- Ministry of National Education, Research and Technology (MENRT)
Ask authors/readers for more resources
In this work, a serie of cyclocoumarol derivatives was designed, synthesized, characterized and studied for their potentialities as selective inhibitors of COX-2. All target compounds have been screened for their anti-inflammatory activity by the assay of PGE2 production. Among them, compound 5d exhibited the most potent inhibitory activity with a PGE2 inhibition compared to NS-398 (79% and 88% respectively) and showed non-inhibitory activity towards the COX-1 enzyme. Docking studies revealed the capacity of this compound to occupy the selective COX-2 cavity establishing additional hydrogen bonds between the oxygen of the methoxy group and the His90 and Arg513 of the binding site of the enzyme. (C) 2018 Elsevier Masson SAS. All rights reserved.
Authors
I am an author on this paper
Click your name to claim this paper and add it to your profile.
Reviews
Recommended
No Data Available