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

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

1
State Key Laboratory of Natural and Biomimetic Drug, Department of Chemical Biology, School of Pharmaceutical Sciences, Peking University, Beijing 100191, China
2
Department of Pharmacology, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China
3
Department of Medicinal Chemistry, School of Pharmaceutical Sciences, Central South University, Changsha, Hunan 410013, China
4
Division of Nephrology, Xiangya Hospital, Central South University, Changsha, Hunan 410008, China
*
Author to whom correspondence should be addressed.
Received: 16 November 2011 / Revised: 10 January 2012 / Accepted: 12 January 2012 / Published: 17 January 2012
(This article belongs to the Section Medicinal Chemistry)
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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 antifibrotic; pirfenidone; fluorofenidone; carbohydrate modified; glucose
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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.

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