Source:http://linkedlifedata.com/resource/pubmed/id/10617082
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| Predicate | Object |
|---|---|
| rdf:type | |
| lifeskim:mentions | |
| pubmed:issue |
24
|
| pubmed:dateCreated |
2000-2-3
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| pubmed:abstractText |
The thiophene-ethyl thiourea (TET) compound N'-[2-(2-thiophene)ethyl]-N'-[2-(5-bromopyridyl)]-thiourea (compound HI-443) was five times more potent than trovirdine, 1250 times more potent than nevirapine, 100 times more potent than delavirdine, 75 times more potent than MKC-442, and 50 times more potent than AZT against the multidrug resistant HIV-1 strain RT-MDR with a V106A mutation. HI-443 was almost as potent against the NNI-resistant HIV-1 strain A17 with a Y181C mutation as it was against HTLV(IIIB). The activity of HI-443 against A17 was ten times more potent than that of trovirdine, 2083 times more potent than that of nevirapine, and 1042 times more potent than that of delavirdine. HI-443 inhibited the replication of the NNI-resistant HIV-1 strain A17 variant with Y181C plus K103N mutations in RT with an IC50 value of 3.3 microM, whereas the IC50 values of trovirdine, nevirapine, and delavirdine were all >100 microM. These findings establish the novel thiophene containing thiourea compound HI-443 as a novel NNI with potent antiviral activity against NNI-sensitive, NNI-resistant and multidrug-resistant strains of HIV-1.
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| pubmed:language |
eng
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| pubmed:journal | |
| pubmed:citationSubset |
IM
|
| pubmed:chemical | |
| pubmed:status |
MEDLINE
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| pubmed:month |
Dec
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| pubmed:issn |
0960-894X
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| pubmed:author | |
| pubmed:issnType |
Print
|
| pubmed:day |
20
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| pubmed:volume |
9
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| pubmed:owner |
NLM
|
| pubmed:authorsComplete |
Y
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| pubmed:pagination |
3411-6
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| pubmed:dateRevised |
2004-11-17
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| pubmed:meshHeading |
pubmed-meshheading:10617082-Anti-HIV Agents,
pubmed-meshheading:10617082-Cells, Cultured,
pubmed-meshheading:10617082-HIV-1,
pubmed-meshheading:10617082-Humans,
pubmed-meshheading:10617082-Microbial Sensitivity Tests,
pubmed-meshheading:10617082-Models, Molecular,
pubmed-meshheading:10617082-Pyridines,
pubmed-meshheading:10617082-Reverse Transcriptase Inhibitors,
pubmed-meshheading:10617082-Thiourea,
pubmed-meshheading:10617082-Virus Replication
|
| pubmed:year |
1999
|
| pubmed:articleTitle |
N'-[2-(2-thiophene)ethyl]-N'-[2-(5-bromopyridyl)] thiourea as a potent inhibitor of NNI-resistant and multidrug-resistant human immunodeficiency virus-1.
|
| pubmed:affiliation |
Drug Discovery Program, and Department of Virology, Hughes Institute, St. Paul, MN 55113, USA.
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| pubmed:publicationType |
Journal Article
|