کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
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1396279 | 1501183 | 2010 | 7 صفحه PDF | دانلود رایگان |

Some pyrogallol and catechol derivatives were synthesized, and their urease inhibitory activity was evaluated by using acetohydroxamic acid (AHA), a well known Helicobacter pylori urease inhibitor, as positive control. The assay results indicate that many compounds have showed potential inhibitory activity against H. pylori urease. 4-(4-Hydroxyphenethyl)phen-1,2-diol (2a) was found to be the most potent urease inhibitor with IC50s of 1.5 ± 0.2 μM for extracted fraction and 4.2 ± 0.3 μM for intact cell, at least 10 times and 20 times lower than those of AHA (IC50 of 17.2 ± 0.9 μM, 100.6 ± 13 μM), respectively. This finding indicate that 2a would be a potential urease inhibitor deserves further research. Molecular dockings of 2a into H. pylori urease active site were performed for understanding the good activity observed.
A series of polyphenols were synthesized and evaluated for inhibitory activity against Helicobacter pylori urease. 4-(4-Hydroxyphenethyl)phen-1,2-diol (2a) was the most potent inhibitors with IC50 = 1.5±μM.Figure optionsDownload as PowerPoint slide
Journal: European Journal of Medicinal Chemistry - Volume 45, Issue 11, November 2010, Pages 5064–5070