Molecules 2012, 17(1), 884-896; doi:10.3390/molecules17010884
Article

Design, Synthesis and Antifibrotic Activities of Carbohydrate- Modified 1-(Substituted aryl)-5-trifluoromethyl-2(1H) Pyridones

1, 1, 1, 2, 2, 2, 3, 4, 4 and 1,* email
Received: 16 November 2011; in revised form: 10 January 2012 / Accepted: 12 January 2012 / Published: 17 January 2012
(This article belongs to the Section Medicinal Chemistry)
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.
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 inhibitory activity than fluorofenidone. Notably, compound 19a demonstrated the highest cell-based inhibitory activity against NIH 3T3 (IC50 = 0.17 mM).
Keywords: antifibrotic; pirfenidone; fluorofenidone; carbohydrate modified; glucose
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MDPI and ACS Style

Lou, Q.; Meng, X.; Lao, Z.; Xuan, L.; Bai, J.; Hou, Q.; Hu, G.; Luo, R.; Tao, L.; Li, Z. Design, Synthesis and Antifibrotic Activities of Carbohydrate- Modified 1-(Substituted aryl)-5-trifluoromethyl-2(1H) Pyridones. Molecules 2012, 17, 884-896.

AMA Style

Lou Q, Meng X, Lao Z, Xuan L, Bai J, Hou Q, Hu G, Luo R, Tao L, Li Z. Design, Synthesis and Antifibrotic Activities of Carbohydrate- Modified 1-(Substituted aryl)-5-trifluoromethyl-2(1H) Pyridones. Molecules. 2012; 17(1):884-896.

Chicago/Turabian Style

Lou, Qinghua; Meng, Xiangbao; Lao, Zhiqi; Xuan, Lingling; Bai, Jinye; Hou, Qi; Hu, Gaoyun; Luo, Renna; Tao, Lijian; Li, Zhongjun. 2012. "Design, Synthesis and Antifibrotic Activities of Carbohydrate- Modified 1-(Substituted aryl)-5-trifluoromethyl-2(1H) Pyridones." Molecules 17, no. 1: 884-896.

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