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Design, Synthesis and Antifibrotic Activities of Carbohydrate-Modified 1-(Substituted aryl)-5-trifluoromethyl-2(1H) Pyridones
Lou, Qinghua1; Meng, Xiangbao1; Lao, Zhiqi1; Xuan, Lingling2,3; Bai, Jinye2,3; Hou, Qi2,3; Hu, Gaoyun4; Luo, Renna5; Tao, Lijian5; Li, Zhongjun1
关键词antifibrotic pirfenidone fluorofenidone carbohydrate modified glucose
刊名MOLECULES
2012
DOI10.3390/molecules17010884
17期:1页:884-896
收录类别SCI
文章类型Article
WOS标题词Science & Technology
类目[WOS]Chemistry, Organic
研究领域[WOS]Chemistry
关键词[WOS]FIBROSIS ; ACETATES ; INFLAMMATION ; PIRFENIDONE ; STRATEGIES ; BEARING ; ANALOGS
英文摘要

Pirfenidone, a pyridone compound, is an effective and novel antifibrotic agent. In this article, we describe the design, synthesis and activity evaluation of novel antifibrotic agents, 1-(substituted aryl)-5-trifluoromethyl-2(1H) pyridones modified with carbohydrate. Most of the title compounds exhibited comparable or better inhibitory activity than fluorofenidone. Notably, compound 19a demonstrated the highest cell-based inhibitory activity against NIH 3T3 (IC50 = 0.17 mM).

语种英语
WOS记录号WOS:000299535700062
引用统计
被引频次:9[WOS]   [WOS记录]     [WOS相关记录]
文献类型期刊论文
条目标识符http://ir.bjmu.edu.cn/handle/400002259/64778
专题北京大学药学院_化学生物学系
作者单位1.Peking Univ, Sch Pharmaceut Sci, Dept Biol Chem, State Key Lab Nat & Biomimet Drug, Beijing 100191, Peoples R China
2.Chinese Acad Med Sci, Inst Mat Med, Dept Pharmacol, Beijing 100050, Peoples R China
3.Peking Union Med Coll, Beijing 100050, Peoples R China
4.Cent S Univ, Sch Pharmaceut Sci, Dept Med Chem, Changsha 410013, Hunan, Peoples R China
5.Cent S Univ, Xiangya Hosp, Div Nephrol, Changsha 410008, Hunan, Peoples R China
推荐引用方式
GB/T 7714
Lou, Qinghua,Meng, Xiangbao,Lao, Zhiqi,et al. Design, Synthesis and Antifibrotic Activities of Carbohydrate-Modified 1-(Substituted aryl)-5-trifluoromethyl-2(1H) Pyridones[J]. MOLECULES,2012,17(1):884-896.
APA Lou, Qinghua.,Meng, Xiangbao.,Lao, Zhiqi.,Xuan, Lingling.,Bai, Jinye.,...&Li, Zhongjun.(2012).Design, Synthesis and Antifibrotic Activities of Carbohydrate-Modified 1-(Substituted aryl)-5-trifluoromethyl-2(1H) Pyridones.MOLECULES,17(1),884-896.
MLA Lou, Qinghua,et al."Design, Synthesis and Antifibrotic Activities of Carbohydrate-Modified 1-(Substituted aryl)-5-trifluoromethyl-2(1H) Pyridones".MOLECULES 17.1(2012):884-896.
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