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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
2
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pubmed:dateCreated |
1991-5-31
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pubmed:abstractText |
A series of dipyridodiazepinones have been shown to be potent inhibitors of human immunodeficiency virus type 1 (HIV-1) reverse transcriptase. The lead compound, BI-RG-587, had a 50% inhibitory concentration of 84 nM against HIV-1 reverse transcriptase activity. This compound reduced plaque formation of HIV-1 in HeLa cells expressing the CD4 receptor by 50% at 15 nM. BI-RG-587 at comparable concentrations inhibited the production of p24 antigen following the acute infection of CEM T-lymphoblastoid cells or primary human monocyte-derived macrophages with HIV-1. No inhibitory effects against HIV-2 or against three picornaviruses were detected. Zidovudine (3'-azido-3'-deoxythymidine [AZT])-susceptible and AZT-resistant isolates of HIV-1 were equally susceptible to BI-RG-587. AZT and BI-RG-587 exhibited synergistic inhibition of HIV-1BRU at all concentrations examined.
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pubmed:grant |
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pubmed:commentsCorrections |
http://linkedlifedata.com/resource/pubmed/commentcorrection/1708976-1689015,
http://linkedlifedata.com/resource/pubmed/commentcorrection/1708976-1701568,
http://linkedlifedata.com/resource/pubmed/commentcorrection/1708976-1968231,
http://linkedlifedata.com/resource/pubmed/commentcorrection/1708976-1969115,
http://linkedlifedata.com/resource/pubmed/commentcorrection/1708976-2114476,
http://linkedlifedata.com/resource/pubmed/commentcorrection/1708976-2201072,
http://linkedlifedata.com/resource/pubmed/commentcorrection/1708976-2334156,
http://linkedlifedata.com/resource/pubmed/commentcorrection/1708976-2413459,
http://linkedlifedata.com/resource/pubmed/commentcorrection/1708976-2466937,
http://linkedlifedata.com/resource/pubmed/commentcorrection/1708976-2467383,
http://linkedlifedata.com/resource/pubmed/commentcorrection/1708976-2538244,
http://linkedlifedata.com/resource/pubmed/commentcorrection/1708976-2586564,
http://linkedlifedata.com/resource/pubmed/commentcorrection/1708976-2821152,
http://linkedlifedata.com/resource/pubmed/commentcorrection/1708976-3047430,
http://linkedlifedata.com/resource/pubmed/commentcorrection/1708976-3299089,
http://linkedlifedata.com/resource/pubmed/commentcorrection/1708976-3299090,
http://linkedlifedata.com/resource/pubmed/commentcorrection/1708976-509527,
http://linkedlifedata.com/resource/pubmed/commentcorrection/1708976-6382953,
http://linkedlifedata.com/resource/pubmed/commentcorrection/1708976-6752972
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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 |
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pubmed:status |
MEDLINE
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pubmed:month |
Feb
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pubmed:issn |
0066-4804
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pubmed:author |
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pubmed:issnType |
Print
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pubmed:volume |
35
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
305-8
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pubmed:dateRevised |
2011-11-17
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pubmed:meshHeading |
pubmed-meshheading:1708976-Antigens, Viral,
pubmed-meshheading:1708976-Antiviral Agents,
pubmed-meshheading:1708976-Cytopathogenic Effect, Viral,
pubmed-meshheading:1708976-Drug Resistance, Microbial,
pubmed-meshheading:1708976-Drug Synergism,
pubmed-meshheading:1708976-HIV-1,
pubmed-meshheading:1708976-HIV-2,
pubmed-meshheading:1708976-HeLa Cells,
pubmed-meshheading:1708976-Humans,
pubmed-meshheading:1708976-Macrophages,
pubmed-meshheading:1708976-Nevirapine,
pubmed-meshheading:1708976-Picornaviridae,
pubmed-meshheading:1708976-Pyridines,
pubmed-meshheading:1708976-Reverse Transcriptase Inhibitors,
pubmed-meshheading:1708976-T-Lymphocytes,
pubmed-meshheading:1708976-Viral Plaque Assay,
pubmed-meshheading:1708976-Zidovudine
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pubmed:year |
1991
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pubmed:articleTitle |
BI-RG-587 is active against zidovudine-resistant human immunodeficiency virus type 1 and synergistic with zidovudine.
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pubmed:affiliation |
University of California, San Diego 92161.
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pubmed:publicationType |
Journal Article,
Research Support, U.S. Gov't, P.H.S.,
Research Support, U.S. Gov't, Non-P.H.S.,
Research Support, Non-U.S. Gov't
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