1256700-78-3Relevant 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
, 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 METHODS AND USES OF 1-(SUBSTITUTED ARYL)-5-TRIFLUOROMETHYL-2-(1H)-PYRIDONE COMPOUNDS AND THEIR SALTS
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, (2012/04/17)
A 1-(substituted aryl)-5-trifluoromethyl-2-(1H)pyridone compounds and pharmaceutical acceptable salts, preparation methods and uses for preparing the drugs for treating fibrosis thereof.