1662710-24-8Relevant articles and documents
Synthesis and biological evaluation of 5-nitropyrimidine-2,4-dione analogues as inhibitors of nitric oxide and iNOS activity
Ma, Liang,He, Linhong,Lei, Lei,Liang, Xiaolin,Lei, Kai,Zhang, Ronghong,Yang, Zhuang,Chen, Lijuan
, p. 296 - 299 (2015/03/04)
Fifty two compounds based on 5-nitropyrimidine-2,4-dione moiety have been synthesized and evaluated for their inhibitory potency on the production of nitric oxide. Among them, compound 36 inhibited the production of nitric oxide (IC50: 8.6 μM) on lipopolysaccharide-induced RAW 264.7 cells and inducible nitric oxide synthase activity (IC50: 6.2 μM), as well as exerted no potential cytotoxicity (IC50 > 80.0 μM). Docking study confirmed that compound 36 was an inducible nitric oxide synthase inhibitor with perfect binding to the active site of inducible nitric oxide synthase. At a dose of 10 mg/kg, oral administration of 36 possessed protective properties in carrageenan-induced paw edema of male ICR mice.