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rdf:type |
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lifeskim:mentions |
umls-concept:C0003451,
umls-concept:C0019704,
umls-concept:C0080194,
umls-concept:C0205314,
umls-concept:C0220781,
umls-concept:C0243071,
umls-concept:C0441655,
umls-concept:C0596988,
umls-concept:C0679622,
umls-concept:C1676059,
umls-concept:C1883254
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pubmed:issue |
5
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pubmed:dateCreated |
2007-5-15
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pubmed:abstractText |
Novel diarylpyrimidines (DAPY), which represent next generation of non-nucleoside reverse transcriptase inhibitors (NNRTIs), were synthesized and their activities against human immunodeficiency virus type I (HIV-1) assessed. Modulations at positions 2 and 6 of the left phenyl ring generated interesting derivatives of TMC278 displaying high potency against wild-type and mutant viruses compared to nevirapine and efavirenz. The pharmacokinetic profile of the best newly synthesized DAPY was evaluated and compared with TMC278 now in phase II clinical trials.
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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 |
May
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pubmed:issn |
0223-5234
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pubmed:author |
pubmed-author:BettensEvaE,
pubmed-author:DemestreChristopheC,
pubmed-author:GuillemontJeromeJ,
pubmed-author:HeeresJanJ,
pubmed-author:HertogsKurtK,
pubmed-author:LewiPaulP,
pubmed-author:MasungiChantalC,
pubmed-author:MordantCélineC,
pubmed-author:PasquierElisabethE,
pubmed-author:PeetersAnikA,
pubmed-author:QueguinerLaurenceL,
pubmed-author:SchmittBenoitB,
pubmed-author:SmeuldersLiesbethL
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pubmed:issnType |
Print
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pubmed:volume |
42
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pubmed:owner |
NLM
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|
pubmed:authorsComplete |
Y
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pubmed:pagination |
567-79
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pubmed:dateRevised |
2008-6-5
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pubmed:meshHeading |
pubmed-meshheading:17223230-Animals,
pubmed-meshheading:17223230-Chromatography, High Pressure Liquid,
pubmed-meshheading:17223230-Dogs,
pubmed-meshheading:17223230-Female,
pubmed-meshheading:17223230-HIV-1,
pubmed-meshheading:17223230-Magnetic Resonance Spectroscopy,
pubmed-meshheading:17223230-Male,
pubmed-meshheading:17223230-Mass Spectrometry,
pubmed-meshheading:17223230-Nitriles,
pubmed-meshheading:17223230-Pyrimidines,
pubmed-meshheading:17223230-Rats,
pubmed-meshheading:17223230-Rats, Wistar,
pubmed-meshheading:17223230-Reverse Transcriptase Inhibitors,
pubmed-meshheading:17223230-Spectrophotometry, Ultraviolet
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pubmed:year |
2007
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pubmed:articleTitle |
Synthesis of novel diarylpyrimidine analogues of TMC278 and their antiviral activity against HIV-1 wild-type and mutant strains.
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|
pubmed:affiliation |
Johnson & Johnson Pharmaceutical Research and Development, Medicinal Chemistry Department, Campus de Maigremont BP315, F-27106 Val de Reuil Cedex, France.
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pubmed:publicationType |
Journal Article
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