Source:http://linkedlifedata.com/resource/pubmed/id/18717581
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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
18
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pubmed:dateCreated |
2008-9-19
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pubmed:abstractText |
A new group of organophosphorus inhibitors of urease, P-methyl phosphinic acids was discovered by using the structure based inhibitor design approach. Several derivatives of the lead compound, aminomethyl(P-methyl)phosphinic acid, were synthesized successfully. Their potency was evaluated in vitro against urease from Bacillus pasteurii and Proteus vulgaris. The studied compounds constitute a group of competitive, reversible inhibitors of bacterial ureases. Obtained thiophosphinic analogues of the most effective structures exhibited kinetic characteristics of potent, slow binding urease inhibitors, with Ki = 170 nM (against B. pasteurii enzyme) for the most active N-( N'-benzyloxycarbonylglycyl)aminomethyl(P-methyl)phosphinothioic acid.
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical | |
pubmed:status |
MEDLINE
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pubmed:month |
Sep
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pubmed:issn |
1520-4804
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pubmed:author | |
pubmed:issnType |
Electronic
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pubmed:day |
25
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pubmed:volume |
51
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
5736-44
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pubmed:meshHeading |
pubmed-meshheading:18717581-Bacillus,
pubmed-meshheading:18717581-Computer-Aided Design,
pubmed-meshheading:18717581-Drug Evaluation, Preclinical,
pubmed-meshheading:18717581-Enzyme Inhibitors,
pubmed-meshheading:18717581-Hydrogen Bonding,
pubmed-meshheading:18717581-Magnetic Resonance Spectroscopy,
pubmed-meshheading:18717581-Models, Molecular,
pubmed-meshheading:18717581-Organophosphorus Compounds,
pubmed-meshheading:18717581-Proteus vulgaris,
pubmed-meshheading:18717581-Spectrometry, Mass, Electrospray Ionization,
pubmed-meshheading:18717581-Urease
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pubmed:year |
2008
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pubmed:articleTitle |
Design, synthesis, and evaluation of novel organophosphorus inhibitors of bacterial ureases.
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pubmed:affiliation |
Department of Bioorganic Chemistry, Faculty of Chemistry, Wroclaw University of Technology, Wyb. Wyspia?skiego 27, 50-370 Wroc?aw, Poland.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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