|
rdf:type |
|
|
lifeskim:mentions |
|
|
pubmed:issue |
15
|
|
pubmed:dateCreated |
2008-7-29
|
|
pubmed:abstractText |
A series of benzyl pyridazinones were evaluated as HIV-1 non-nucleoside reverse transcriptase inhibitors (NNRTIs). Several members of this series showed good activity against the wild-type virus and NNRTI-resistant viruses. The binding of inhibitor 5a to HIV-RT was analyzed by surface plasmon resonance spectroscopy. Pharmacokinetic studies of 5a in rat and dog demonstrated that this compound has good oral bioavailability in animal species. The crystal structure of a complex between HIV-RT and inhibitor 4c is also described.
|
|
pubmed:language |
eng
|
|
pubmed:journal |
|
|
pubmed:citationSubset |
IM
|
|
pubmed:chemical |
|
|
pubmed:status |
MEDLINE
|
|
pubmed:month |
Aug
|
|
pubmed:issn |
1464-3405
|
|
pubmed:author |
pubmed-author:DunnJames PJP,
pubmed-author:DuntenPeteP,
pubmed-author:ElworthyTodd RTR,
pubmed-author:HanXiaochunX,
pubmed-author:HarrisSeth FSF,
pubmed-author:HeilekGabrielleG,
pubmed-author:HirschfeldDonald RDR,
pubmed-author:HoggJ HeatherJH,
pubmed-author:HuberWalterW,
pubmed-author:KaiserAnn CAC,
pubmed-author:KerteszDenis JDJ,
pubmed-author:KimWoongkiW,
pubmed-author:KlumppKlausK,
pubmed-author:MirzadeganTaranehT,
pubmed-author:RoepelMichael GMG,
pubmed-author:SaitoY DavidYD,
pubmed-author:SilvaTania M P CTM,
pubmed-author:SwallowStevenS,
pubmed-author:SweeneyZachary KZK,
pubmed-author:TracyJahari LJL,
pubmed-author:VillasenorArmandoA,
pubmed-author:VoraHaritH,
pubmed-author:YuLiL,
pubmed-author:ZhouAmy SAS
|
|
pubmed:issnType |
Electronic
|
|
pubmed:day |
1
|
|
pubmed:volume |
18
|
|
pubmed:owner |
NLM
|
|
pubmed:authorsComplete |
Y
|
|
pubmed:pagination |
4352-4
|
|
pubmed:meshHeading |
pubmed-meshheading:18632268-Animals,
pubmed-meshheading:18632268-Dogs,
pubmed-meshheading:18632268-Drug Resistance, Viral,
pubmed-meshheading:18632268-HIV Reverse Transcriptase,
pubmed-meshheading:18632268-Inhibitory Concentration 50,
pubmed-meshheading:18632268-Molecular Structure,
pubmed-meshheading:18632268-Pyridazines,
pubmed-meshheading:18632268-Rats,
pubmed-meshheading:18632268-Reverse Transcriptase Inhibitors,
pubmed-meshheading:18632268-Structure-Activity Relationship
|
|
pubmed:year |
2008
|
|
pubmed:articleTitle |
Discovery and optimization of pyridazinone non-nucleoside inhibitors of HIV-1 reverse transcriptase.
|
|
pubmed:affiliation |
Roche Palo Alto LLC, 3431 Hillview Avenue, Palo Alto, CA 94304, USA. zachary.sweeney@roche.com
|
|
pubmed:publicationType |
Journal Article
|
