Synthesis of new imidazolones and their biological evaluation as COX-2 inhibitors

RESEARCH JOURNAL OF PHARMACEUTICAL BIOLOGICAL AND CHEMICAL SCIENCES(2018)

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摘要
New series of imidazolones were designed and synthesized and evaluated against both COX-1 and COX-2 enzymes. Based on the outcome of in vitro COX assay most of the derivatives showed selective COX-2 inhibitory activity specifically compounds Ila and IVb with IC50 values 0.12 and 0.19 mu M compared to celecoxib with IC50 value of 0.05 mu M and diclofenac sodium with IC50 value of 0.8 mu M on COX-2 enzyme.
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关键词
Imidazolone,COX-1,COX-2,Synthesis,anti-inflammatory
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