Source:http://linkedlifedata.com/resource/pubmed/id/17931865
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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
23
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pubmed:dateCreated |
2007-11-6
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pubmed:abstractText |
A series of potent novel 8-hydroxy-3,4-dihydropyrrolo[1,2-a]pyrazine-1(2H)-one HIV-1 integrase inhibitors was identified. These compounds inhibited the strand transfer process of HIV-1 integrase and viral replication in cells. Compound 12 is active against replication of HIV-1 in cell culture with a CIC(95) of 0.31microM. Further SAR exploration led to the preparation of pseudosymmetrical tricyclic pyrrolopyrazine inhibitors 23 and 24 with further improvement in antiviral activity.
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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 |
Dec
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pubmed:issn |
1464-3405
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pubmed:author |
pubmed-author:AnariM RezaMR,
pubmed-author:FelockPeter JPJ,
pubmed-author:FisherThorsten ETE,
pubmed-author:GabryelskiLori JLJ,
pubmed-author:HazudaDaria JDJ,
pubmed-author:KimBoyoungB,
pubmed-author:KochanskyChristopher JCJ,
pubmed-author:LyleTerry ATA,
pubmed-author:SchleifWilliam AWA,
pubmed-author:StaasDonnette DDD,
pubmed-author:VaccaJoseph PJP,
pubmed-author:WaiJohn SJS,
pubmed-author:YoungSteven DSD,
pubmed-author:ZradaMatthew MMM
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pubmed:issnType |
Electronic
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pubmed:day |
1
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pubmed:volume |
17
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
6511-5
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pubmed:meshHeading | |
pubmed:year |
2007
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pubmed:articleTitle |
8-Hydroxy-3,4-dihydropyrrolo[1,2-a]pyrazine-1(2H)-one HIV-1 integrase inhibitors.
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pubmed:affiliation |
Department of Medicinal Chemistry, Merck Research Laboratories, West Point, PA 19486, USA. thor_fisher@merck.com
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pubmed:publicationType |
Journal Article,
Comparative Study
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