1256782-99-6

Basic information

• Product Name: 5-trifluoromethyl-(1-(2-((2-hydroxyl)ethyl)amino)benzyl)pyridine-2(1H)-one
• Synonyms: 5-trifluoromethyl-(1-(2-((2-hydroxyl)ethyl)amino)benzyl)pyridine-2(1H)-one
• CAS NO: 1256782-99-6
• Molecular Weight: 312.292
• Mol File: 1256782-99-6.mol
• Article Data: 3

Chemical Properties

• CAS DataBase Reference: 5-trifluoromethyl-(1-(2-((2-hydroxyl)ethyl)amino)benzyl)pyridine-2(1H)-one(CAS DataBase Reference)
• NIST Chemistry Reference: 5-trifluoromethyl-(1-(2-((2-hydroxyl)ethyl)amino)benzyl)pyridine-2(1H)-one(1256782-99-6)
• EPA Substance Registry System: 5-trifluoromethyl-(1-(2-((2-hydroxyl)ethyl)amino)benzyl)pyridine-2(1H)-one(1256782-99-6)

Safety Data

• Hazardous Substances Data: 1256782-99-6(Hazardous Substances Data)

Upstream product

• 612-23-7 2-nitrobenzyl chloride 
• 3958-60-9 2-nitrophenylmethyl bromide 
• 1256782-97-4 1-(2-aminobenzyl)-5-trifluoromethyl-2(1H)-pyridone 
• 107-07-3 2-chloro-ethanol 
• 33252-63-0 5-(trifluoromethyl)-2(1H)-pyridone 
• 1256782-96-3 1-(2-nitrobenzyl)-5-(trifluoromethyl)pyridin-2(1H)-one 
• 1365919-82-9 2-chloro-5-trifluoromethyl-pyridine 

Downstream Products

• 1256783-00-2 1-(2-((2-(piperazin-1-yl)ethyl)amino)benzyl)-5-(trifluoromethyl)pyridin-2(1H)-one 
• 1256783-06-8 1-(2-((2-chloroethyl)amino)benzyl)-5-(trifluoromethyl)pyridin-2(1H)-one 
• 1256783-01-3 1-(2-((2-(4-methylpiperazin-1-yl)ethyl)amino)benzyl)-5-(trifluoromethyl)pyridin-2(1H)-one 

Relevant articles and documents

Discovery of 1-(4-((3-(4-methylpiperazin-1-yl)propyl)amino)benzyl)-5-(trifluoromethyl)pyridin-2(1H)-one, an orally active multi-target agent for the treatment of diabetic nephropathy

Oxidative stress, inflammation and fibrosis can cause irreversible damage on cell structure and function of kidney and are key pathological factors in Diabetic Nephropathy (DN). Therefore, multi-target agents are urgently need for the clinical treatment of DN. Using Pirfenidone as a lead compound and based on the previous research, two novel series (5-trifluoromethyl)-2(1H)-pyridone analogs were designed and synthesized. SAR of (5-trifluoromethyl)-2(1H)-pyridone derivatives containing nitrogen heterocyclic ring have been established for in vitro potency. In addition, compound 8, a novel agent that act on multiple targets of anti-DN with IC50 of 90 μM in NIH3T3 cell lines, t1/2 of 4.89 ± 1.33 h in male rats and LD50 > 2000 mg/kg in mice, has been advanced to preclinical studies as an oral treatment for DN.

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.