Source:http://linkedlifedata.com/resource/pubmed/id/18707089
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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
18
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pubmed:dateCreated |
2008-9-23
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pubmed:abstractText |
Analogues of the 4"-benzoyl-ureido-TSAO derivative (1) modified at different positions have been prepared and evaluated against wild-type strains of HCMV and murine cytomegalovirus (MCMV) in cell culture. In addition, the activity of the most active derivatives against several drug-resistant HCMV mutants has been determined. A stringent structure-antiviral activity relationship was observed for the 4"-benzoylureido- TSAO derivatives for which the concomitant presence of a highly lipophilic substituent at both 2'- and 5'-positions was required to fully preserve the antihuman cytomegalovirus efficacy. Time-of-addition studies and HCMV immediately early and early gene expression studies revealed a target at the time of viral DNA synthesis, although direct inhibition of HCMV-encoded DNA polymerase could not be observed in cell-free assays. Lack of cross-resistance against a broad variety of mutant HCMV strains points to an antiviral target that is different from those drugs that are currently approved for clinical use.
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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 |
Sep
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pubmed:issn |
1520-4804
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pubmed:author | |
pubmed:issnType |
Electronic
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pubmed:day |
25
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pubmed:volume |
51
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
5823-32
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pubmed:meshHeading |
pubmed-meshheading:18707089-Antiviral Agents,
pubmed-meshheading:18707089-Cell Line,
pubmed-meshheading:18707089-Cytomegalovirus,
pubmed-meshheading:18707089-Humans,
pubmed-meshheading:18707089-Magnetic Resonance Spectroscopy,
pubmed-meshheading:18707089-Microbial Sensitivity Tests,
pubmed-meshheading:18707089-Spectrometry, Mass, Electrospray Ionization,
pubmed-meshheading:18707089-Structure-Activity Relationship,
pubmed-meshheading:18707089-Thymidine,
pubmed-meshheading:18707089-Urea
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pubmed:year |
2008
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pubmed:articleTitle |
4"-Benzoylureido-TSAO derivatives as potent and selective non-nucleoside HCMV inhibitors. Structure-activity relationship and mechanism of antiviral action.
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pubmed:affiliation |
Instituto de Química Médica (CSIC), Juan de Cierva 3, E-28006 Madrid, Spain.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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