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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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/

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spelling	doaj-31f4ec9d74564042bf329c2b19e35c832020-11-24T22:10:44ZengMDPI AGMolecules1420-30492012-01-0117188489610.3390/molecules17010884Design, Synthesis and Antifibrotic Activities of Carbohydrate- Modified 1-(Substituted aryl)-5-trifluoromethyl-2(1H) PyridonesLijian TaoZhongjun LiRenna LuoGaoyun HuQi HouZhiqi LaoLingling XuanJinye BaiXiangbao MengQinghua LouPirfenidone, 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).http://www.mdpi.com/1420-3049/17/1/884/antifibroticpirfenidonefluorofenidonecarbohydrate modifiedglucose
collection	DOAJ
language	English
format	Article
sources	DOAJ
author	Lijian Tao Zhongjun Li Renna Luo Gaoyun Hu Qi Hou Zhiqi Lao Lingling Xuan Jinye Bai Xiangbao Meng Qinghua Lou
spellingShingle	Lijian Tao Zhongjun Li Renna Luo Gaoyun Hu Qi Hou Zhiqi Lao Lingling Xuan Jinye Bai Xiangbao Meng Qinghua Lou Design, Synthesis and Antifibrotic Activities of Carbohydrate- Modified 1-(Substituted aryl)-5-trifluoromethyl-2(1H) Pyridones Molecules antifibrotic pirfenidone fluorofenidone carbohydrate modified glucose
author_facet	Lijian Tao Zhongjun Li Renna Luo Gaoyun Hu Qi Hou Zhiqi Lao Lingling Xuan Jinye Bai Xiangbao Meng Qinghua Lou
author_sort	Lijian Tao
title	Design, Synthesis and Antifibrotic Activities of Carbohydrate- Modified 1-(Substituted aryl)-5-trifluoromethyl-2(1H) Pyridones
title_short	Design, Synthesis and Antifibrotic Activities of Carbohydrate- Modified 1-(Substituted aryl)-5-trifluoromethyl-2(1H) Pyridones
title_full	Design, Synthesis and Antifibrotic Activities of Carbohydrate- Modified 1-(Substituted aryl)-5-trifluoromethyl-2(1H) Pyridones
title_fullStr	Design, Synthesis and Antifibrotic Activities of Carbohydrate- Modified 1-(Substituted aryl)-5-trifluoromethyl-2(1H) Pyridones
title_full_unstemmed	Design, Synthesis and Antifibrotic Activities of Carbohydrate- Modified 1-(Substituted aryl)-5-trifluoromethyl-2(1H) Pyridones
title_sort	design, synthesis and antifibrotic activities of carbohydrate- modified 1-(substituted aryl)-5-trifluoromethyl-2(1h) pyridones
publisher	MDPI AG
series	Molecules
issn	1420-3049
publishDate	2012-01-01
description	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).
topic	antifibrotic pirfenidone fluorofenidone carbohydrate modified glucose
url	http://www.mdpi.com/1420-3049/17/1/884/
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Design, Synthesis and Antifibrotic Activities of Carbohydrate- Modified 1-(Substituted aryl)-5-trifluoromethyl-2(1H) Pyridones

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