Source:http://linkedlifedata.com/resource/pubmed/id/18046963
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
5
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pubmed:dateCreated |
2007-11-30
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pubmed:abstractText |
We designed and synthesized novel 2,3-disubstituted quinazolin-4(3H)-ones by microwave technique and characterized them by spectral analysis. Synthesized compounds were screened for cytotoxicity and for antiviral activity against influenza A (H1N1, H3N2 and H5N1), severe acute respiratory syndrome corona, dengue, yellow fever, Venezuelan equine encephalitis (VEE), Rift Valley fever, and Tacaribe viruses in cell culture. A neutral red uptake assay was used to determine 50% virus-inhibitory concentrations (EC50) of test compounds and their 50% cytotoxicity concentration (CC50) in uninfected Madin-Darby canine kidney, Vero, and Vero 76 cells; selectivity indices (ratio of CC50 to EC50) were derived from the data. The compound 4-(6,8-dibromo-4-oxo-2-phenyl quinazolin-3(4H)-yl)-N-(4,5-dimethyloxazol-2yl) benzenesulphonamide 15 inhibited the replication of avian influenza (H5N1) virus (EC50 = 8.4 microg/ml, CC50 > 100 microg/ml, SI > 11.9) as did 4-(6-bromo-4oxo-2phenylquinazolin-3(4H)-yl) benzene]sulphonamide 5 (EC50 = 3 microg/ml, CC50 = 32 microg/ml, SI = 11). Compound 5 was also moderately active against VEE and Tacaribe viruses. The methodology described in this report is applicable for rapid synthesis of many compounds with potential antiviral properties.
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pubmed:grant | |
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:issn |
0956-3202
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:volume |
18
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
301-5
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pubmed:meshHeading |
pubmed-meshheading:18046963-Animals,
pubmed-meshheading:18046963-Antiviral Agents,
pubmed-meshheading:18046963-Cercopithecus aethiops,
pubmed-meshheading:18046963-Dogs,
pubmed-meshheading:18046963-Microbial Sensitivity Tests,
pubmed-meshheading:18046963-Microwaves,
pubmed-meshheading:18046963-Molecular Structure,
pubmed-meshheading:18046963-Quinazolinones,
pubmed-meshheading:18046963-Sulfonamides,
pubmed-meshheading:18046963-Vero Cells,
pubmed-meshheading:18046963-Virus Replication,
pubmed-meshheading:18046963-Viruses
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pubmed:year |
2007
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pubmed:articleTitle |
Novel 3-sulphonamido-quinazolin-4(3H)-one derivatives: microwave-assisted synthesis and evaluation of antiviral activities against respiratory and biodefense viruses.
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pubmed:affiliation |
Arulmigu Kalasalingam College of Pharmacy, Krishnankoil-626190, India. periyasamyselvam2001@yahoo.co.in
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pubmed:publicationType |
Journal Article,
Research Support, N.I.H., Extramural
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