13159-76-7Relevant academic research and scientific papers
Synthesis and evaluation of N-analogs of 1,2-diarylethane as Helicobacter pylori urease inhibitors
Xiao, Zhu-Ping,Shi, Wei-Kang,Wang, Peng-Fei,Wei, Wei,Zeng, Xiao-Tong,Zhang, Ji-Rong,Zhu, Na,Peng, Miao,Peng, Bin,Lin, Xiao-Yi,Ouyang, Hui,Peng, Xiao-Chun,Wang, Guang-Cheng,Zhu, Hai-Liang
, p. 4508 - 4513 (2015/08/03)
Therapies based on urease inhibition are now seriously considered as the first line of treatment for infections caused by Helicobacter pylori. However, the present inhibitors are ineffective or unstable in highly acidic gastric juice. Here, we report a series of benzylanilines as effective inhibitors of H. pylori urease. Out of the obtained twenty-one compounds, N-(3,4-dihydroxybenzyl)-4-nitroaniline (4) was evaluated in detail and shows promising features for development as anti-H. pylori agent. Excellent potency against urease in both cell-free extract and intact cell was observed at low concentrations of 4 (IC50 = 0.62 ± 0.04 and 1.92 ± 0.09 μM), which showed over 29- and 54-fold increase in potency with respect to the positive control AHA. The SAR analysis revealed that protection of 3,4-dihydroxy group of 4 as methoxy or changes of 4-NO2 will result in a moderate to dramatic decrease in potency.
In(OTf)3 catalyzed N-benzylation of amines utilizing benzyl alcohols in water
Yang, Jin-Ming,Jiang, Ran,Wu, Lin,Xu, Xiao-Ping,Wang, Shun-Yi,Ji, Shun-Jun
, p. 7988 - 7994 (2013/08/23)
An In(OTf)3-catalyzed N-benzylation of amines utilizing benzyl alcohols through direct C-O bond activation has been reported. The reaction was performed in water without any base, additive, ligand or inert gas protection to afford the chem-selective mono- or bis-alkylated aromatic amines in good to excellent yields.
Sodium borohydride on wet clay: Solvent-free reductive amination of carbonyl compounds using microwaves
Varma, Rajender S.,Dahiya, Rajender
, p. 6293 - 6298 (2007/10/03)
A solvent-flee reductive amination of carbonyl compounds by wet montmorillonite K 10 clay supported sodium borohydride is described; microwave irradiation facilitates the procedure.
