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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 |
1993-2-19
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pubmed:abstractText |
In an ongoing effort to develop novel nonnucleoside, specific human immunodeficiency virus type 1 (HIV-1) reverse transcriptase (RT) inhibitors, a series of 3-[(pyridylmethyl)amino]- and 3-[(phenylmethyl)amino]-2-pyridinone derivatives was synthesized and tested for HIV-1 RT inhibitory activity. The more potent compounds have a 2'-methoxy group and 4'- and/or 5'-aliphatic substituents on the pyridyl and phenyl rings. Several of the more potent compounds were also evaluated for antiviral activity in MT-4 cell culture. From this series of compounds, 3-[N-[(5-ethyl-2-methoxy-6-methyl-3-pyridyl)methyl]amino]-5-ethyl-6- methylpyridin-2(1H)-one (6) was selected for clinical evaluation.
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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 |
Jan
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pubmed:issn |
0022-2623
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pubmed:author |
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pubmed:issnType |
Print
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pubmed:day |
22
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pubmed:volume |
36
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pubmed:owner |
NLM
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pubmed:authorsComplete |
N
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pubmed:pagination |
249-55
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pubmed:dateRevised |
2007-11-15
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pubmed:meshHeading |
pubmed-meshheading:7678654-Aminopyridines,
pubmed-meshheading:7678654-Animals,
pubmed-meshheading:7678654-Antiviral Agents,
pubmed-meshheading:7678654-Cells, Cultured,
pubmed-meshheading:7678654-HIV Reverse Transcriptase,
pubmed-meshheading:7678654-Haplorhini,
pubmed-meshheading:7678654-Pyridones,
pubmed-meshheading:7678654-Rats,
pubmed-meshheading:7678654-Reverse Transcriptase Inhibitors,
pubmed-meshheading:7678654-Structure-Activity Relationship
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pubmed:year |
1993
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pubmed:articleTitle |
Synthesis and evaluation of 2-pyridinone derivatives as specific HIV-1 reverse transcriptase inhibitors. 3. Pyridyl and phenyl analogs of 3-aminopyridin-2(1H)-one.
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pubmed:affiliation |
Merck Research Laboratories, West Point, Pennsylvania 19486.
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pubmed:publicationType |
Journal Article
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