Design, synthesis, biological evaluation and molecular docking of curcumin analogues as antioxidant, cyclooxygenase inhibitory and anti-inflammatory agents

Selvam, C. ; Jachak, Sanjay M. ; Thilagavathi, Ramasamy ; Chakraborti, Asit. K. (2005) Design, synthesis, biological evaluation and molecular docking of curcumin analogues as antioxidant, cyclooxygenase inhibitory and anti-inflammatory agents Bioorganic & Medicinal Chemistry Letters, 15 (7). pp. 1793-1797. ISSN 0960-894X

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Official URL: http://www.sciencedirect.com/science/article/pii/S...

Related URL: http://dx.doi.org/10.1016/j.bmcl.2005.02.039

Abstract

Curcuminoids were isolated from Curcuma longa and their pyrazole and isoxazole analogues were synthesized and evaluated for antioxidant, COX-1/COX-2 inhibitory and anti-inflammatory activities. The designed analogues significantly enhance COX-2/COX-1 selectivity and possess significant anti-inflammatory activity in carrageenan induced rat paw edema assay. Pyrazole, isoxazole analogues of curcumin (4 and 7) exhibited higher antioxidant activity than trolox. Molecular docking study revealed the binding orientations of curcumin analogues in the active sites of COX and thereby helps to design novel potent inhibitors.

Item Type:Article
Source:Copyright of this article belongs to Elsevier Science.
Keywords:Curcuminoids; Pyrazole Analogues; Isoxazole Analogues; Cox-1; Cox-2; Anti-Inflammatory Activity; Antioxidant Activity
ID Code:100639
Deposited On:19 Jan 2017 11:58
Last Modified:19 Jan 2017 11:58

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