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rdf:type |
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lifeskim:mentions |
umls-concept:C0001128,
umls-concept:C0021467,
umls-concept:C0021469,
umls-concept:C0205460,
umls-concept:C0220781,
umls-concept:C0220825,
umls-concept:C0233820,
umls-concept:C0243072,
umls-concept:C0600115,
umls-concept:C0678594,
umls-concept:C0917728,
umls-concept:C1883254,
umls-concept:C2603343
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|
pubmed:issue |
5
|
|
pubmed:dateCreated |
2011-3-28
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|
pubmed:abstractText |
New quinolonyl diketo acid compounds bearing various substituents at position 6 of the quinolone scaffold were designed and synthesized as potential HIV-1 integrase inhibitors. These new compounds were evaluated for their antiviral and anti-integrase activity and showed inhibitory potency similar to that of 6-bromide analog 2. Molecular modeling and docking studies were performed to rationalize these data and to provide a detailed understanding of the mechanism of inhibition for this class of compounds.
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pubmed:language |
eng
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pubmed:journal |
|
|
pubmed:citationSubset |
IM
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|
pubmed:chemical |
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|
pubmed:status |
MEDLINE
|
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pubmed:month |
May
|
|
pubmed:issn |
1768-3254
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|
pubmed:author |
pubmed-author:CardonaChristelleC,
pubmed-author:CauvinChristineC,
pubmed-author:GeorgesBenoîtB,
pubmed-author:GuiguenAllanA,
pubmed-author:HevesiLászlóL,
pubmed-author:Le VanKietK,
pubmed-author:MbembaGladysG,
pubmed-author:MichauxCatherineC,
pubmed-author:MouscadetJean-FrançoisJF,
pubmed-author:Van LintCarineC,
pubmed-author:VandurmPierreP,
pubmed-author:WoutersJohanJ
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pubmed:copyrightInfo |
Copyright © 2011 Elsevier Masson SAS. All rights reserved.
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pubmed:issnType |
Electronic
|
|
pubmed:volume |
46
|
|
pubmed:owner |
NLM
|
|
pubmed:authorsComplete |
Y
|
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pubmed:pagination |
1749-56
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pubmed:meshHeading |
pubmed-meshheading:21385662-Anti-HIV Agents,
pubmed-meshheading:21385662-Catalytic Domain,
pubmed-meshheading:21385662-Dose-Response Relationship, Drug,
pubmed-meshheading:21385662-Drug Design,
pubmed-meshheading:21385662-HIV,
pubmed-meshheading:21385662-HIV Integrase,
pubmed-meshheading:21385662-HIV Integrase Inhibitors,
pubmed-meshheading:21385662-Keto Acids,
pubmed-meshheading:21385662-Models, Molecular,
pubmed-meshheading:21385662-Molecular Structure,
pubmed-meshheading:21385662-Quinolones,
pubmed-meshheading:21385662-Stereoisomerism,
pubmed-meshheading:21385662-Structure-Activity Relationship
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pubmed:year |
2011
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pubmed:articleTitle |
Synthesis, biological evaluation and molecular modeling studies of quinolonyl diketo acid derivatives: new structural insight into the HIV-1 integrase inhibition.
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pubmed:affiliation |
Département de Chimie, Facultés Universitaires Notre-Dame de la Paix (FUNDP), B-Namur 5000, Belgium. pierre.vandurm@fundp.ac.be
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
|
