Synthesis and biological evaluations of novel isoxazoles and furoxan derivative as anti-inflammatory agents

被引：35
作者：
Abdelall, Eman K. A. [1 ]
机构：
[1] Beni Suef Univ, Fac Pharm, Dept Pharmaceut Organ Chem, Bani Suwayf 62514, Egypt
来源：
BIOORGANIC CHEMISTRY | 2020年 / 94卷
关键词：
Ant-inflammatory; Celecoxib; Isoxazoles; Furoxans; Pyrazoles; PYRAZOLE CYCLIZATION; INHIBITORS; 5-LIPOXYGENASE; CYCLOOXYGENASE; COX-2;
D O I：
10.1016/j.bioorg.2019.103441
中图分类号：
Q5 [生物化学]; Q7 [分子生物学];
学科分类号：
071010 ; 081704 ;
摘要：
Novel isoxazoles (10, 12a&b, 15a-c) and the furoxan derivative (14) have been prepared as new safe antiinflammatory agents from the hydroximoyl 9. All compounds were evaluated for COX-1\COX-2 and most of them showed promising selectivity. The furoxan derivative 14 gave 59% inhibitory activity using carrageenan induced paw rat edema model. Ulcer index experiment and histo-pathological study of stomach samples were also included. Also the proposed binding mode of certain newly synthesized compounds with COX-2 isoform was briefly discussed.
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页数：12
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