SYNTHESIS OF 4-[5-(SUBSTITUTED ARYL)-4,5-DIHYDRO-1H-PYRAZOL-3-YL]-3-PHENYL-SYDNONES AS ANTIINFLAMMATORY, ANTIARTHRITIC AND ANALGESIC AGENTS

被引：24
|
作者：
SATYANARAYANA, K [1 ]
RAO, MNA [1 ]
机构：
[1] KASTURBA MED COLL & HOSP,COLL PHARMACEUT SCI,DEPT PHARMACEUT CHEM,MANIPAL 576119,INDIA
来源：
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 1995年 / 30卷 / 7-8期
关键词：
SYDNONE; PYRAZOLINE; ANTIINFLAMMATORY ACTIVITY; ANTIARTHRITIC ACTIVITY; ANALGESIC ACTIVITY;
D O I：
10.1016/0223-5234(96)88280-8
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
4-[1-Oxo-3-(substituted aryl)-2-propenyl]-3-phenylsydnones were condensed with hydrazine to yield fourteen 4-[5-(substituted aryl)-4,5-dihydro-1H-pyrazol-3-yl]-3-phenylsydnones. Four compounds have shown antiinflammatory activity in carrageenen-induced edema assay in rats and six compounds have shown analgesic activity in acetic-acid-induced writhing assay in mice at a dosage of 100 mg/kg po. The antiinflammatory activity of these compounds was less than the positive controls phenylbutazone and ibuprofen. However, compound 25 has shown more analgesic activity than aspirin (ED(50), 28.3 vs 81.4 mg/kg respectively, po). Two compounds have shown antiarthritic activity in adjuvant-induced arthritis in rats. The ulcerogenicity of active compounds was less than phenylbutazone.
引用
收藏
页码：641 / 645
页数：5
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