16290-66-7Relevant academic research and scientific papers
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.
Discovery and development of a small molecule library with lumazine synthase inhibitory activity
Talukdar, Arindam,Breen, Meghan,Bacher, Adelbert,Illarionov, Boris,Fischer, Markus,Georg, Gunda,Ye, Qi-Zhuang,Cushman, Mark
experimental part, p. 5123 - 5134 (2009/12/24)
(Chemical Equation Presented) (E)-5-Nitro-6-(2-hydroxystyryl)pyrimidine-2, 4(1H,3H)-dione (9) was identified as a novel inhibitor of Schizosaccharomyces pombe lumazine synthase by high-throughput screening of a 100000 compound library. The Ki o
