کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1396279 1501183 2010 7 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
The synthesis, structure and activity evaluation of pyrogallol and catechol derivatives as Helicobacter pylori urease inhibitors
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
The synthesis, structure and activity evaluation of pyrogallol and catechol derivatives as Helicobacter pylori urease inhibitors
چکیده انگلیسی

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

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: European Journal of Medicinal Chemistry - Volume 45, Issue 11, November 2010, Pages 5064–5070
نویسندگان
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