923688-20-4Relevant 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
Chen, Jun,Peng, Zhangzhe,Lu, Miaomiao,Xiong, Xuan,Chen, Zhuo,Li, Qianbin,Cheng, Zeneng,Jiang, Dejian,Tao, Lijian,Hu, Gaoyun
supporting information, p. 222 - 229 (2017/12/28)
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.
PREPARATION OF 1-(SUBSTITUTED BENZYL)-5-TRIFLUOROMETHYL-2(1H)PYRIDONE COMPOUNDS AND SALTS THEREOF AND THEIR APPLICATIONS
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Page/Page column 6, (2012/06/01)
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.