3-Trifluoromethylpyrazolones derived nucleosides: Synthesis and antiviral evaluation.
Identifieur interne : 000D74 ( Main/Exploration ); précédent : 000D73; suivant : 000D753-Trifluoromethylpyrazolones derived nucleosides: Synthesis and antiviral evaluation.
Auteurs : Ayman M S. Ahmed [Égypte] ; Reham A I. Abou-Elkhair [Égypte] ; Alaa M. El-Torky [Égypte] ; Abdalla E A. Hassan [Égypte]Source :
- Nucleosides, nucleotides & nucleic acids [ 1532-2335 ] ; 2019.
Descripteurs français
- KwdFr :
- Antiviraux (pharmacologie), Antiviraux (synthèse chimique), Conception de médicament, Coronavirus du syndrome respiratoire du Moyen-Orient (), Hepacivirus (), Humains, Influenzavirus A (), Nucléosides (pharmacologie), Nucléosides (synthèse chimique), Pyrazolones (), Relation structure-activité, Réplication virale (), Structure moléculaire, Virus de l'hépatite B (), Virus de la dengue (), Virus respiratoires syncytiaux ().
- MESH :
- pharmacologie : Antiviraux, Nucléosides.
- synthèse chimique : Antiviraux, Nucléosides.
- Conception de médicament, Coronavirus du syndrome respiratoire du Moyen-Orient, Hepacivirus, Humains, Influenzavirus A, Pyrazolones, Relation structure-activité, Réplication virale, Structure moléculaire, Virus de l'hépatite B, Virus de la dengue, Virus respiratoires syncytiaux.
English descriptors
- KwdEn :
- Antiviral Agents (chemical synthesis), Antiviral Agents (pharmacology), Dengue Virus (drug effects), Drug Design, Hepacivirus (drug effects), Hepatitis B virus (drug effects), Humans, Influenzavirus A (drug effects), Middle East Respiratory Syndrome Coronavirus (drug effects), Molecular Structure, Nucleosides (chemical synthesis), Nucleosides (pharmacology), Pyrazolones (chemistry), Respiratory Syncytial Viruses (drug effects), Structure-Activity Relationship, Virus Replication (drug effects).
- MESH :
- chemical , chemical synthesis : Antiviral Agents, Nucleosides.
- chemical , chemistry : Pyrazolones.
- chemical , pharmacology : Antiviral Agents, Nucleosides.
- drug effects : Dengue Virus, Hepacivirus, Hepatitis B virus, Influenzavirus A, Middle East Respiratory Syndrome Coronavirus, Respiratory Syncytial Viruses, Virus Replication.
- Drug Design, Humans, Molecular Structure, Structure-Activity Relationship.
Abstract
Dengue (DENV) viral infection is a global public health problem that infrequently develops life threatening diseases such as dengue hemorrhagic fever (DFS) and dengue shock syndrome (DSS). Middle East respiratory syndrome coronavirus (MERS-CoV) is a highly pathogenic human corona virus with 38% fatality rate of infected patients. A series of 4-arylhydrazono-5-trifluoromethyl-pyrazolones, their ribofuranosyl, and 5'-deoxyribofuranosyl nucleosides were synthesized, geometry optimized using Density functional theory (DFT), and evaluated for their antiviral activity. 2-Nitrophenylhydrazonopyra-zolone derivative 5 showed significant activity against MERS-CoV (EC50 = 4.6 μM). The nucleoside analog 8 showed moderate activity against DENV-2 (EC50 = 10 μM), while the activity was abolished with the corresponding 5'-deoxyribonucleoside analogs. The identified hits in this study set this category of compounds for further future optimizations.
DOI: 10.1080/15257770.2019.1591445
PubMed: 30929566
Affiliations:
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Le document en format XML
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Ahmed</name><affiliation wicri:level="1"><nlm:affiliation>a Applied Nucleic Acids Research Center , Zagazig University , Zagazig , Egypt.</nlm:affiliation><country xml:lang="fr">Égypte</country><wicri:regionArea>a Applied Nucleic Acids Research Center , Zagazig University , Zagazig </wicri:regionArea><wicri:noRegion>Zagazig </wicri:noRegion></affiliation></author><author><name sortKey="Abou Elkhair, Reham A I" sort="Abou Elkhair, Reham A I" uniqKey="Abou Elkhair R" first="Reham A I" last="Abou-Elkhair">Reham A I. Abou-Elkhair</name><affiliation wicri:level="1"><nlm:affiliation>a Applied Nucleic Acids Research Center , Zagazig University , Zagazig , Egypt.</nlm:affiliation><country xml:lang="fr">Égypte</country><wicri:regionArea>a Applied Nucleic Acids Research Center , Zagazig University , Zagazig </wicri:regionArea><wicri:noRegion>Zagazig </wicri:noRegion></affiliation></author><author><name sortKey="El Torky, Alaa M" sort="El Torky, Alaa M" uniqKey="El Torky A" first="Alaa M" last="El-Torky">Alaa M. El-Torky</name><affiliation wicri:level="1"><nlm:affiliation>a Applied Nucleic Acids Research Center , Zagazig University , Zagazig , Egypt.</nlm:affiliation><country xml:lang="fr">Égypte</country><wicri:regionArea>a Applied Nucleic Acids Research Center , Zagazig University , Zagazig </wicri:regionArea><wicri:noRegion>Zagazig </wicri:noRegion></affiliation></author><author><name sortKey="Hassan, Abdalla E A" sort="Hassan, Abdalla E A" uniqKey="Hassan A" first="Abdalla E A" last="Hassan">Abdalla E A. Hassan</name><affiliation wicri:level="1"><nlm:affiliation>a Applied Nucleic Acids Research Center , Zagazig University , Zagazig , Egypt.</nlm:affiliation><country xml:lang="fr">Égypte</country><wicri:regionArea>a Applied Nucleic Acids Research Center , Zagazig University , Zagazig </wicri:regionArea><wicri:noRegion>Zagazig </wicri:noRegion></affiliation></author></analytic><series><title level="j">Nucleosides, nucleotides & nucleic acids</title><idno type="eISSN">1532-2335</idno><imprint><date when="2019" type="published">2019</date></imprint></series></biblStruct></sourceDesc></fileDesc><profileDesc><textClass><keywords scheme="KwdEn" xml:lang="en"><term>Antiviral Agents (chemical synthesis)</term><term>Antiviral Agents (pharmacology)</term><term>Dengue Virus (drug effects)</term><term>Drug Design</term><term>Hepacivirus (drug effects)</term><term>Hepatitis B virus (drug effects)</term><term>Humans</term><term>Influenzavirus A (drug effects)</term><term>Middle East Respiratory Syndrome Coronavirus (drug effects)</term><term>Molecular Structure</term><term>Nucleosides (chemical synthesis)</term><term>Nucleosides (pharmacology)</term><term>Pyrazolones (chemistry)</term><term>Respiratory Syncytial Viruses (drug effects)</term><term>Structure-Activity Relationship</term><term>Virus Replication (drug effects)</term></keywords><keywords scheme="KwdFr" xml:lang="fr"><term>Antiviraux (pharmacologie)</term><term>Antiviraux (synthèse chimique)</term><term>Conception de médicament</term><term>Coronavirus du syndrome respiratoire du Moyen-Orient ()</term><term>Hepacivirus ()</term><term>Humains</term><term>Influenzavirus A ()</term><term>Nucléosides (pharmacologie)</term><term>Nucléosides (synthèse chimique)</term><term>Pyrazolones ()</term><term>Relation structure-activité</term><term>Réplication virale ()</term><term>Structure moléculaire</term><term>Virus de l'hépatite B ()</term><term>Virus de la dengue ()</term><term>Virus respiratoires syncytiaux ()</term></keywords><keywords scheme="MESH" type="chemical" qualifier="chemical synthesis" xml:lang="en"><term>Antiviral Agents</term><term>Nucleosides</term></keywords><keywords scheme="MESH" type="chemical" qualifier="chemistry" xml:lang="en"><term>Pyrazolones</term></keywords><keywords scheme="MESH" type="chemical" qualifier="pharmacology" xml:lang="en"><term>Antiviral Agents</term><term>Nucleosides</term></keywords><keywords scheme="MESH" qualifier="drug effects" xml:lang="en"><term>Dengue Virus</term><term>Hepacivirus</term><term>Hepatitis B virus</term><term>Influenzavirus A</term><term>Middle East Respiratory Syndrome Coronavirus</term><term>Respiratory Syncytial Viruses</term><term>Virus Replication</term></keywords><keywords scheme="MESH" qualifier="pharmacologie" xml:lang="fr"><term>Antiviraux</term><term>Nucléosides</term></keywords><keywords scheme="MESH" qualifier="synthèse chimique" xml:lang="fr"><term>Antiviraux</term><term>Nucléosides</term></keywords><keywords scheme="MESH" xml:lang="en"><term>Drug Design</term><term>Humans</term><term>Molecular Structure</term><term>Structure-Activity Relationship</term></keywords><keywords scheme="MESH" xml:lang="fr"><term>Conception de médicament</term><term>Coronavirus du syndrome respiratoire du Moyen-Orient</term><term>Hepacivirus</term><term>Humains</term><term>Influenzavirus A</term><term>Pyrazolones</term><term>Relation structure-activité</term><term>Réplication virale</term><term>Structure moléculaire</term><term>Virus de l'hépatite B</term><term>Virus de la dengue</term><term>Virus respiratoires syncytiaux</term></keywords></textClass></profileDesc></teiHeader><front><div type="abstract" xml:lang="en">Dengue (DENV) viral infection is a global public health problem that infrequently develops life threatening diseases such as dengue hemorrhagic fever (DFS) and dengue shock syndrome (DSS). Middle East respiratory syndrome coronavirus (MERS-CoV) is a highly pathogenic human corona virus with 38% fatality rate of infected patients. A series of 4-arylhydrazono-5-trifluoromethyl-pyrazolones, their ribofuranosyl, and 5'-deoxyribofuranosyl nucleosides were synthesized, geometry optimized using Density functional theory (DFT), and evaluated for their antiviral activity. 2-Nitrophenylhydrazonopyra-zolone derivative 5 showed significant activity against MERS-CoV (EC<sub>50</sub> = 4.6 μM). The nucleoside analog 8 showed moderate activity against DENV-2 (EC<sub>50</sub> = 10 μM), while the activity was abolished with the corresponding 5'-deoxyribonucleoside analogs. The identified hits in this study set this category of compounds for further future optimizations.</div></front></TEI><affiliations><list><country><li>Égypte</li></country></list><tree><country name="Égypte"><noRegion><name sortKey="Ahmed, Ayman M S" sort="Ahmed, Ayman M S" uniqKey="Ahmed A" first="Ayman M S" last="Ahmed">Ayman M S. Ahmed</name></noRegion><name sortKey="Abou Elkhair, Reham A I" sort="Abou Elkhair, Reham A I" uniqKey="Abou Elkhair R" first="Reham A I" last="Abou-Elkhair">Reham A I. Abou-Elkhair</name><name sortKey="El Torky, Alaa M" sort="El Torky, Alaa M" uniqKey="El Torky A" first="Alaa M" last="El-Torky">Alaa M. El-Torky</name><name sortKey="Hassan, Abdalla E A" sort="Hassan, Abdalla E A" uniqKey="Hassan A" first="Abdalla E A" last="Hassan">Abdalla E A. Hassan</name></country></tree></affiliations></record>Pour manipuler ce document sous Unix (Dilib)
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