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

被引：279
作者：
Selvam, C
Jachak, SM
Thilagavathi, R
Chakraborti, AK
机构：
[1] NIPER, Dept Nat Prod, SAS Nagar 160062, Punjab, India
[2] NIPER, Dept Med Chem, SAS Nagar 160062, Punjab, India
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2005年 / 15卷 / 07期
关键词：
curcuminoids; pyrazole analogues; isoxazole analogues; COX-1; COX-2; anti-inflammatory activity; antioxidant activity;
D O I：
10.1016/j.bmcl.2005.02.039
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
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. (c) 2005 Elsevier Ltd. All rights reserved.
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收藏
页码：1793 / 1797
页数：5
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