1256782-95-2

Upstream product

• 1256782-84-9 5-trifluoromethyl-(1-(4-amino)benzyl)pyridine-2(1H)-one 
• 64-19-7 acetic acid 
• 1365919-82-9 2-chloro-5-trifluoromethyl-pyridine 
• 108-24-7 acetic anhydride 
• 100-11-8 1-bromomethyl-4-nitro-benzene 
• 33252-63-0 5-(trifluoromethyl)-2(1H)-pyridone 
• 923688-20-4 5-trifluoromethyl-(1-(4-nitro)benzyl)pyridine-2(1H)-one 

Relevant academic research and scientific papers

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

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 IC50 of 0.08 mmol/L about 34 times of AKF-PD. The SAR of pyridone derivatives as anti-fibrosis agents was also discussed.

PREPARATION OF 1-(SUBSTITUTED BENZYL)-5-TRIFLUOROMETHYL-2(1H)PYRIDONE COMPOUNDS AND SALTS THEREOF AND THEIR APPLICATIONS

1-(substituted benzyl)-5-trifluoromethyl-2(1H)pyridone compounds and their pharmaceutical acceptable salts are disclosed. The preparation methods of the compounds and their salts and the use of the same for preparing the medicaments for treating fibrosis are also disclosed. New pyridine compounds and their salts are obtained from trifluoromethyl pyridone as starting material.