1025814-16-7Relevant 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.
Inversion of the reactivity of benzyl bromides in reactions with anilines in dioxane and its mixtures with dimethyl sulfoxide. Experimental proof for isoparametric relationships
Shpan'ko
, p. 1010 - 1013 (2007/10/03)
Analysis of the structure-reactivity cross correlations shows the existence of isoparametric relationships in the reaction of Y-substituted benzyl bromides with X-substituted anilines in dioxane and 2, 3, and 5 M solutions of dimethyl sulfoxide in dioxane
