Synthesis and structure-activity relationship of 5-substituent-2(1H)-pyridone derivatives as anti-fibrosis agents

Bioorganic & Medicinal Chemistry Letters
Jun ChenGao Yun Hu

Abstract

Pyridone compounds, such as pirfenidone (PFD) and fluorofenidone (AKF-PD), are multi-target anti-fibrotic agents. Using PFD and AKF-PD as the leading compounds, two series of novel (5-substituent)-2(1H)-pyridone compounds were synthesized with the purpose of maintaining multi-targeting property and overcoming the drawbacks of fast metabolism. These derivatives demonstrated good proliferation inhibiting activity against NIH3T3 cells by MTT assay with AKF-PD as the positive control. Compound 5b exhibited a high potent of anti-fibrosis with a IC(50) of 0.08 mmol/L about 34 times of AKF-PD. The SAR of pyridone derivatives as anti-fibrosis agents was also discussed.

References

Feb 28, 2002·British Journal of Pharmacology·Stevo MirkovicLindsay Brown
Mar 31, 2007·Cell Death and Differentiation·J-C Dussaule, C Chatziantoniou

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Citations

Oct 31, 2019·Brazilian Journal of Medical and Biological Research = Revista Brasileira De Pesquisas Médicas E Biológicas·Hui YangWangbin Ning
May 2, 2015·The Journal of Organic Chemistry·Dong-Ling WangSong Ye
Jan 27, 2017·Journal of Medicinal Chemistry·Yi-Min LiuJing-Ping Liou

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