期刊
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
卷 31, 期 -, 页码 54-60出版社
TAYLOR & FRANCIS LTD
DOI: 10.1080/14756366.2016.1201815
关键词
Anti-inflammatory; cyclooxygenase-2 inhibitors; 1; 5-diarylpyrazole
A new series of 1,5-diarylpyrazoles 10a-l was designed and synthesized for evaluation as COX inhibitors and as anti-inflammatory agents. All compounds were more selective for COX-2 isozyme and showed good in vivo anti-inflammatory activity. Compound 10e was the most COX-2 selective compound (S.I.=10.67) and the most potent anti-inflammatory derivative (ED50=46mol/kg) which is approximately 11-folds more potent than ibuprofen (ED50=499mol/kg) and had 2/3 potency of celecoxib (ED50=31mol/kg). All compounds were less ulcerogenic (ulcer indexes=1.20-4.61) than ibuprofen (ulcer index=20.25) and comparable to celecoxib (ulcer index=2.90).
作者
我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。
推荐
暂无数据