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- Title
Synthesis and Biologic Evaluation of Substituted 5-methyl-2-phenyl-1H-pyrazol-3(2H)-one Derivatives as Selective COX-2 Inhibitors: Molecular Docking Study.
- Authors
Dube, Pritam N.; Bule, Shweta S.; Mokale, Santosh N.; Kumbhare, Manoj R.; Dighe, Pravin R.; Ushir, Yogesh V.
- Abstract
The present study reported the synthesis and biologic evaluation of new pyrazolone derivatives for COX-2 inhibitory activities and investigated in vivo for their anti-inflammatory activities using carrageenan-induced rat paw edema model as well as in vitro using HRBC membrane stabilization and protein denaturation method. Eight derivatives showed pronounced COX-2 inhibition, and 5a, 5d, and 5f exhibited the highest COX-2 inhibition. The derivatives were further evaluated for antioxidant activity wherein 5a and 5b showed potent free radical-scavenging activity against DPPH, nitric oxide, and hydrogen peroxide radicals. Molecular docking study revealed the binding orientations of pyrazolone derivatives into the active sites of COX-2 and thereby helps to design the potent inhibitors.
- Subjects
PYRAZOLONES; MOLECULAR docking; CYCLOOXYGENASE 2 inhibitors; CARRAGEENANS; DENATURATION of proteins; ANTIOXIDANTS; NITRIC oxide
- Publication
Chemical Biology & Drug Design, 2014, Vol 84, Issue 4, p409
- ISSN
1747-0277
- Publication type
Article
- DOI
10.1111/cbdd.12324