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Keywords = fluorofenidone

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13 pages, 279 KB  
Article
Design, Synthesis and Antifibrotic Activities of Carbohydrate- Modified 1-(Substituted aryl)-5-trifluoromethyl-2(1H) Pyridones
by Qinghua Lou, Xiangbao Meng, Zhiqi Lao, Lingling Xuan, Jinye Bai, Qi Hou, Gaoyun Hu, Renna Luo, Lijian Tao and Zhongjun Li
Molecules 2012, 17(1), 884-896; https://doi.org/10.3390/molecules17010884 - 17 Jan 2012
Cited by 22 | Viewed by 7616
Abstract
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 [...] Read more.
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). Full article
(This article belongs to the Section Medicinal Chemistry)
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