2. Academic Validation
  3. 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

  • Molecules. 2012 Jan 17;17(1):884-96. doi: 10.3390/molecules17010884.
Qinghua Lou 1,  Xiangbao Meng,  Zhiqi Lao,  Lingling Xuan,  Jinye Bai,  Qi Hou,  Gaoyun Hu,  Renna Luo,  Lijian Tao,  Zhongjun Li
Affiliations

Affiliation

  • 1 State Key Laboratory of Natural and Biomimetic Drug, Department of Chemical Biology, School of Pharmaceutical Sciences, Peking University, Beijing 100191, China.
PMID: 22252504 DOI: 10.3390/molecules17010884
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 (IC(50) = 0.17 mM).

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