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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Autores principales: Lou, Qinghua, Meng, Xiangbao, Lao, Zhiqi, Xuan, Lingling, Bai, Jinye, Hou, Qi, Hu, Gaoyun, Luo, Renna, Tao, Lijian, Li, Zhongjun
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2012
Materias:
Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6269014/
https://www.ncbi.nlm.nih.gov/pubmed/22252504
http://dx.doi.org/10.3390/molecules17010884
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author Lou, Qinghua
Meng, Xiangbao
Lao, Zhiqi
Xuan, Lingling
Bai, Jinye
Hou, Qi
Hu, Gaoyun
Luo, Renna
Tao, Lijian
Li, Zhongjun
author_facet Lou, Qinghua
Meng, Xiangbao
Lao, Zhiqi
Xuan, Lingling
Bai, Jinye
Hou, Qi
Hu, Gaoyun
Luo, Renna
Tao, Lijian
Li, Zhongjun
author_sort Lou, Qinghua
collection PubMed
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 (IC(50) = 0.17 mM).
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spelling pubmed-62690142018-12-11 Design, Synthesis and Antifibrotic Activities of Carbohydrate- Modified 1-(Substituted aryl)-5-trifluoromethyl-2(1H) Pyridones Lou, Qinghua Meng, Xiangbao Lao, Zhiqi Xuan, Lingling Bai, Jinye Hou, Qi Hu, Gaoyun Luo, Renna Tao, Lijian Li, Zhongjun Molecules Article 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 (IC(50) = 0.17 mM). MDPI 2012-01-17 /pmc/articles/PMC6269014/ /pubmed/22252504 http://dx.doi.org/10.3390/molecules17010884 Text en © 2012 by the authors; licensee MDPI, Basel, Switzerland. http://creativecommons.org/licenses/by/3.0/ This article is an open-access article distributed under the terms and conditions of the Creative Commons Attribution license (http://creativecommons.org/licenses/by/3.0/).
spellingShingle Article
Lou, Qinghua
Meng, Xiangbao
Lao, Zhiqi
Xuan, Lingling
Bai, Jinye
Hou, Qi
Hu, Gaoyun
Luo, Renna
Tao, Lijian
Li, Zhongjun
Design, Synthesis and Antifibrotic Activities of Carbohydrate- Modified 1-(Substituted aryl)-5-trifluoromethyl-2(1H) Pyridones
title 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_short 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
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6269014/
https://www.ncbi.nlm.nih.gov/pubmed/22252504
http://dx.doi.org/10.3390/molecules17010884
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