Next Article in Journal
Studies on 3-Oxoalkanenitriles: Novel Rearrangement Reactions Observed in Studies of the Chemistry of 3-Heteroaroyl-3-Oxoalkanenitriles as Novel Routes to 2-Dialkylaminopyridines
Previous Article in Journal
Novel Benzothiazole, Benzimidazole and Benzoxazole Derivatives as Potential Antitumor Agents: Synthesis and Preliminary in Vitro Biological Evaluation
Article Menu

Export Article

Open AccessArticle
Molecules 2012, 17(1), 884-896; https://doi.org/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)
Full-Text   |   PDF [279 KB, uploaded 18 June 2014]   |  

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). View Full-Text
Keywords: antifibrotic; pirfenidone; fluorofenidone; carbohydrate modified; glucose antifibrotic; pirfenidone; fluorofenidone; carbohydrate modified; glucose
Figures

Graphical abstract

This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).
SciFeed

Share & Cite This Article

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.

Show more citation formats Show less citations formats

Related Articles

Article Metrics

Article Access Statistics

1

Comments

[Return to top]
Molecules EISSN 1420-3049 Published by MDPI AG, Basel, Switzerland RSS E-Mail Table of Contents Alert
Back to Top