Source:http://linkedlifedata.com/resource/pubmed/id/20801557
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
11
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pubmed:dateCreated |
2010-10-11
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pubmed:abstractText |
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 IC(50)s of 1.5±0.2 ?M for extracted fraction and 4.2±0.3 ?M for intact cell, at least 10 times and 20 times lower than those of AHA (IC(50) of 17.2±0.9 ?M, 100.6±13 ?M), 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.
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Catechols,
http://linkedlifedata.com/resource/pubmed/chemical/Enzyme Inhibitors,
http://linkedlifedata.com/resource/pubmed/chemical/Pyrogallol,
http://linkedlifedata.com/resource/pubmed/chemical/Urease,
http://linkedlifedata.com/resource/pubmed/chemical/catechol
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pubmed:status |
MEDLINE
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pubmed:month |
Nov
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pubmed:issn |
1768-3254
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pubmed:author | |
pubmed:copyrightInfo |
Copyright © 2010 Elsevier Masson SAS. All rights reserved.
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pubmed:issnType |
Electronic
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pubmed:volume |
45
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
5064-70
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pubmed:meshHeading |
pubmed-meshheading:20801557-Catechols,
pubmed-meshheading:20801557-Enzyme Inhibitors,
pubmed-meshheading:20801557-Helicobacter pylori,
pubmed-meshheading:20801557-Models, Molecular,
pubmed-meshheading:20801557-Pyrogallol,
pubmed-meshheading:20801557-Structure-Activity Relationship,
pubmed-meshheading:20801557-Urease
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pubmed:year |
2010
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pubmed:articleTitle |
The synthesis, structure and activity evaluation of pyrogallol and catechol derivatives as Helicobacter pylori urease inhibitors.
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pubmed:affiliation |
Key Laboratory of Hunan Forest Products and Chemical Industry Engineering, Jishou University, Jishou 416000, PR China. xiaozhuping2005@163.com
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pubmed:publicationType |
Journal Article
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