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

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

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 exhi...

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Bibliographic Details
Main Authors: Lijian Tao, Zhongjun Li, Renna Luo, Gaoyun Hu, Qi Hou, Zhiqi Lao, Lingling Xuan, Jinye Bai, Xiangbao Meng, Qinghua Lou
Format: Article
Language:English
Published: MDPI AG 2012-01-01
Series:Molecules
Subjects:
antifibrotic
pirfenidone
fluorofenidone
carbohydrate modified
glucose
Online Access:http://www.mdpi.com/1420-3049/17/1/884/
Description
Summary: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).
ISSN:1420-3049

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