Source:http://linkedlifedata.com/resource/pubmed/id/10389655
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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
2
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pubmed:dateCreated |
1999-8-11
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pubmed:abstractText |
Efficient synthetic routes of 2-amino-4-(omega-hydroxyalkylamino)pyrimidine derivatives were investigated in relation to the anti-influenza virus activity of these compounds. The derivatives in which cyclobutyl and cyclopentyl groups were introduced to the beta-position of the aminoalkyl group (especially the cyclobutyl group substituted by a phenylalkyl group at the 3'-position) resulted in improved antiviral potency: i.e. an average 50% effective concentration for inhibition of plaque formation (EC50, microM) of 0.1-0.01 microM for both types A and B influenza virus. The antiviral efficacies were in the order of amino group > hydroxyiminomethyl group > halogen substitution at the 5-position, and chlorine or methoxy group > hydrogen at the 6-position of the pyrimidine ring. The antiviral indices of these compounds were 2-6 with respect to the 50% inhibitory concentration for cell proliferation (IC50, microM) for growing cells, but > 500 to > 10(4) with respect to the IC50 for stationary cells, indicating that these compounds may be efficacious for the topical treatment of influenza virus infection.
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical | |
pubmed:status |
MEDLINE
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pubmed:month |
Jun
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pubmed:issn |
0166-3542
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pubmed:author | |
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 |
121-37
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pubmed:dateRevised |
2004-11-17
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pubmed:meshHeading |
pubmed-meshheading:10389655-Animals,
pubmed-meshheading:10389655-Antiviral Agents,
pubmed-meshheading:10389655-Cell Line,
pubmed-meshheading:10389655-Humans,
pubmed-meshheading:10389655-Inhibitory Concentration 50,
pubmed-meshheading:10389655-Microbial Sensitivity Tests,
pubmed-meshheading:10389655-Orthomyxoviridae,
pubmed-meshheading:10389655-Pyrimidines,
pubmed-meshheading:10389655-Structure-Activity Relationship
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pubmed:year |
1999
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pubmed:articleTitle |
Synthesis and anti-influenza virus activity of novel pyrimidine derivatives.
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pubmed:affiliation |
Institute for Drug Development, Nesco Company, AZWELL Inc., Ibaragi, Japan.
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pubmed:publicationType |
Journal Article
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