Output ID:  1100008403392
Category:  期刊论文
Journal Article Title:  :  Development of benzoxazole deoxybenzoin oxime and acyloxylamine derivatives targeting innate immune sensors and xanthine oxidase for treatment of gout
Abstract:  Both the inhibition of inflammatory flares and the treatment of hyperuricemia itself are included in the management of gout. Extending our efforts to development of gout therapy, two series of benzoxazole deoxybenzoin oxime derivatives as inhibitors of innate immune sensors and xanthine oxidase (XOD) were discovered in improving hyperuricemia and acute gouty arthritis. In vitro studies revealed that most compounds not only suppressed XOD activity, but blocked activations of NOD-like receptor (NLRP3) inflammasome and Toll-like receptor 4 (TLR4) signaling pathway. More importantly, (E)-1-(6-methoxybenzo[d]oxazol-2-yl)-2-(4-methoxyphenyl)ethanone oxime (5d) exhibited anti-hyperuricemic and antiacute gouty arthritis activities through regulating XOD, NLRP3 and TLR4. Compound 5d may serve as a tool compound for further design of anti-gout drugs targeting both innate immune sensors and XOD.
Keywords:  Xanthine oxidase; NOD-like receptor 3; Toll-like receptor 4; Anti-hyperuricemia; Gout 
Authors:  Huang Jun; Zhou Zehao; Zhou Mengze; Miao Mingxing; Li Huanqiu*; Hu Qinghua*
Journal Name:  Bioorganic & Medicinal Chemistry 
Status:  Published
Publication Date/Period:  2018-5-1 
Issue No.: 
Volume No.:  26 
Pages:  1653-1664 
Indexed by:  scie
DOI:  10.1016/j.bmc.2018.02.013
Times Cited:  7
Related Links:  View     
Last update date:  2021/03/15 23:31:03 
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