Synthesis of new pyrazoles and pyrozolo [3,4-b] pyridines as anti-inflammatory agents by inhibition of COX-2 enzyme.

Bioorganic Chemistry(2019)

引用 45|浏览1
暂无评分
摘要
New pyrazoles and pyrazolo pyridines were synthesized and their structure was confirmed by elemental analyses as well as IR, 1H NMR, 13C NMR, and mass spectral data. All the newly synthesized derivatives were evaluated in vitro for inhibitory activity against COX-1 and COX-2 enzymes and their IC50 values were calculated, most of the derivatives showed good inhibitory activity with derivatives IVb, IVh and IVJ showing inhibitory activity better than celecoxib. Moreover, the eight most potent derivatives IVa, IVb, IVc, IVd, IVe, IVh, IVJ, and IVL were selected for in vivo assay to measure their effect on paw edema in rates and their ulcerogenic effect. Compounds IVa, IVb and IVc were found to be the most active and selective as COX-2 inhibitors and most effective in protection from edema they also have lowest ulcerogenic effect among all derivatives.
更多
查看译文
关键词
UEGWCDLTZGCHBM-KKZZFGNYSA-N,CZOQWVIYSDRPQC-JQJXEDNGSA-N,LATHQULJDQGVCW-CTYXJAJWSA-N,MGYOXNQMRJWAMP-QWOYOHQZSA-N,IKSWDNARYJRWHF-UHFFFAOYSA-N,QCPSMEDFGFSBSZ-UHFFFAOYSA-N
AI 理解论文
溯源树
样例
生成溯源树,研究论文发展脉络
Chat Paper
正在生成论文摘要