CovidV2, Main, Exploration, bibRecord, 001683

Novel 3-sulphonamido-quinazolin-4(3H)-one derivatives : microwave-assisted synthesis and evaluation of antiviral activities against respiratory and biodefense viruses

Identifieur interne : 001683 ( Main/Exploration ); précédent : 001682; suivant : 001684

Novel 3-sulphonamido-quinazolin-4(3H)-one derivatives : microwave-assisted synthesis and evaluation of antiviral activities against respiratory and biodefense viruses

Auteurs : Periyasamy Selvam [Inde] ; Paulchamy Vijayalakshimi [Inde] ; Donald F. Smee [États-Unis] ; Brian B. Gowen [États-Unis] ; Justin G. Julander [États-Unis] ; Craig W. Day [États-Unis] ; Dale L. Barnard [États-Unis]

Source :

Antiviral chemistry & chemotherapy [ 0956-3202 ] ; 2007.

RBID : Pascal:08-0040513

Descripteurs français

Pascal (Inist)
- Virus encéphalite équine Venezuela, Evaluation, Antiviral, Voie respiratoire, Synthèse chimique, Virus Tacaribe, Dérivé de la quinazolinone, Influenzavirus A(H5N1).

English descriptors

KwdEn :
- Antiviral, Chemical synthesis, Evaluation, Influenzavirus A(H5N1), Respiratory tract, Tacaribe virus, Venezuelan equine encephalomyelitis virus.

Abstract

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 ug/ml, CC₅₀>100 μg/ml, Sl>11.9) as did 4-(6-bromo-4oxo-2phenylquinazolin-3(4H)-yl) benzene]sulphonamide 5 (EC₅₀=3 (μg/ml, CC₅₀= 32 μg/ml, Sl=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.

Affiliations:

Inde, États-Unis
Utah

Links toward previous steps (curation, corpus...)

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to stream PascalFrancis, to step Checkpoint: 000031
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Le document en format XML

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<keywords scheme="Pascal" xml:lang="fr"><term>Virus encéphalite équine Venezuela</term>
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<front><div type="abstract" xml:lang="en">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 (EC<sub>50</sub>
) of test compounds and their 50% cytotoxicity concentration (CC<sub>50</sub>
) in uninfected Madin-Darby canine kidney, Vero, and Vero 76 cells; selectivity indices (ratio of CC<sub>50</sub>
 to EC<sub>50</sub>
) 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 (EC<sub>50</sub>
=8.4 ug/ml, CC<sub>50</sub>
>100 μg/ml, Sl>11.9) as did 4-(6-bromo-4oxo-2phenylquinazolin-3(4H)-yl) benzene]sulphonamide 5 (EC<sub>50</sub>
=3 (μg/ml, CC<sub>50</sub>
= 32 μg/ml, Sl=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.</div>
</front>
</TEI>
<affiliations><list><country><li>Inde</li>
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<tree><country name="Inde"><noRegion><name sortKey="Selvam, Periyasamy" sort="Selvam, Periyasamy" uniqKey="Selvam P" first="Periyasamy" last="Selvam">Periyasamy Selvam</name>
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<country name="États-Unis"><region name="Utah"><name sortKey="Smee, Donald F" sort="Smee, Donald F" uniqKey="Smee D" first="Donald F." last="Smee">Donald F. Smee</name>
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<name sortKey="Gowen, Brian B" sort="Gowen, Brian B" uniqKey="Gowen B" first="Brian B." last="Gowen">Brian B. Gowen</name>
<name sortKey="Julander, Justin G" sort="Julander, Justin G" uniqKey="Julander J" first="Justin G." last="Julander">Justin G. Julander</name>
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Novel 3-sulphonamido-quinazolin-4(3H)-one derivatives : microwave-assisted synthesis and evaluation of antiviral activities against respiratory and biodefense viruses

Novel 3-sulphonamido-quinazolin-4(3H)-one derivatives : microwave-assisted synthesis and evaluation of antiviral activities against respiratory and biodefense viruses

Source :

Descripteurs français

English descriptors

Abstract

Links toward previous steps (curation, corpus...)

Le document en format XML

Pour manipuler ce document sous Unix (Dilib)

Pour mettre un lien sur cette page dans le réseau Wicri