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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
15
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pubmed:dateCreated |
2009-7-14
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pubmed:abstractText |
A novel class of tetrahydro-pyrazinopyrimidine-2-carboxamides have been identified as HIV-1 integrase inhibitors. Optimization of the initial lead culminated in the discovery of a series of compounds with high potency on the enzyme and an antiviral cell-based activity equivalent to that showed by Raltegravir, the first in class HIV-1 integrase inhibitor.
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pubmed:language |
eng
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pubmed:journal |
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pubmed:citationSubset |
IM
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pubmed:chemical |
|
|
pubmed:status |
MEDLINE
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pubmed:month |
Aug
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pubmed:issn |
1464-3405
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pubmed:author |
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pubmed:issnType |
Electronic
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pubmed:day |
1
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pubmed:volume |
19
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
4245-9
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pubmed:meshHeading |
pubmed-meshheading:19523819-Animals,
pubmed-meshheading:19523819-Cell Line,
pubmed-meshheading:19523819-Chemistry, Pharmaceutical,
pubmed-meshheading:19523819-Drug Design,
pubmed-meshheading:19523819-HIV Integrase Inhibitors,
pubmed-meshheading:19523819-Humans,
pubmed-meshheading:19523819-Inhibitory Concentration 50,
pubmed-meshheading:19523819-Magnetic Resonance Spectroscopy,
pubmed-meshheading:19523819-Models, Chemical,
pubmed-meshheading:19523819-Nitrogen,
pubmed-meshheading:19523819-Pyrazines,
pubmed-meshheading:19523819-Pyrimidines,
pubmed-meshheading:19523819-Rats,
pubmed-meshheading:19523819-Stereoisomerism,
pubmed-meshheading:19523819-Structure-Activity Relationship
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pubmed:year |
2009
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pubmed:articleTitle |
N-(4-Fluorobenzyl)-3-hydroxy-9,9-dimethyl-4-oxo-6,7,8,9-tetrahydro-4H-pyrazino[1,2-a]pyrimidine-2-carboxamides a novel class of potent HIV-1 integrase inhibitors.
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pubmed:affiliation |
Departments of Medicinal Chemistry and Drug Metabolism IRBM-MRL, Via Pontina, Km 30.600, 00040 Pomezia (RM), Italy. alessia_petrocchi@merck.com
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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