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rdf:type |
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lifeskim:mentions |
|
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pubmed:issue |
4
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pubmed:dateCreated |
2008-2-21
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pubmed:databankReference |
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pubmed:abstractText |
A new generation of HIV-1 protease inhibitors encompassing a tertiary-alcohol-based transition-state mimic has been developed. By elongation of the core structure of recently reported inhibitors with two carbon atoms and by varying the P1' group of the compounds, efficient inhibitors were obtained with Ki down to 2.3 nM and EC50 down to 0.17 microM. Two inhibitor-enzyme X-ray structures are reported.
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pubmed:commentsCorrections |
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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 |
Feb
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pubmed:issn |
0022-2623
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pubmed:author |
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pubmed:issnType |
Print
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pubmed:day |
28
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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 |
1053-7
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pubmed:dateRevised |
2008-5-20
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pubmed:meshHeading |
pubmed-meshheading:18215014-Alcohols,
pubmed-meshheading:18215014-Binding Sites,
pubmed-meshheading:18215014-Carbamates,
pubmed-meshheading:18215014-Cell Line,
pubmed-meshheading:18215014-Crystallography, X-Ray,
pubmed-meshheading:18215014-HIV Protease Inhibitors,
pubmed-meshheading:18215014-HIV-1,
pubmed-meshheading:18215014-Humans,
pubmed-meshheading:18215014-Hydrazines,
pubmed-meshheading:18215014-Imidazoles,
pubmed-meshheading:18215014-Models, Molecular,
pubmed-meshheading:18215014-Molecular Mimicry,
pubmed-meshheading:18215014-Oxadiazoles,
pubmed-meshheading:18215014-Pyridines,
pubmed-meshheading:18215014-Stereoisomerism
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pubmed:year |
2008
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pubmed:articleTitle |
Two-carbon-elongated HIV-1 protease inhibitors with a tertiary-alcohol-containing transition-state mimic.
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pubmed:affiliation |
Department of Medicinal Chemistry, Organic Pharmaceutical Chemistry, BMC, Uppsala University, Box 574, SE-751 23 Uppsala, Sweden.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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