Novel Hypoglycemic Dihydropyridones Serendipitously Discovered from O-versus C-Alkylation in The Synthesis of VMAT2 Antagonists
Identifieur interne : 003068 ( Main/Exploration ); précédent : 003067; suivant : 003069Novel Hypoglycemic Dihydropyridones Serendipitously Discovered from O-versus C-Alkylation in The Synthesis of VMAT2 Antagonists
Auteurs : Yuli Xie [États-Unis] ; Anthony Raffo [États-Unis] ; Masanori Ichise [États-Unis] ; Shixian Deng [États-Unis] ; Paul E. Harris [États-Unis] ; Donald W. Landry [États-Unis]Source :
- Bioorganic & medicinal chemistry letters [ 0960-894X ] ; 2008.
Abstract
Vesicular monoamine transporter type 2 (VMAT2) is a newly emerging target for both diagnostic and therapeutic applications in diabetes mellitus. In pursuit of novel VMAT2 antagonists, we identified a potent hypoglycemic agent with a novel dihydropyridone scaffold. Several analogs were designed and synthesized. A preliminary structure activity relationship (SARs) showed that the dihydropyridone scaffold is required for the activity.
Url:
DOI: 10.1016/j.bmcl.2008.07.129
PubMed: 18752945
PubMed Central: 3632391
Affiliations:
Links toward previous steps (curation, corpus...)
- to stream Pmc, to step Corpus: 000D42
- to stream Pmc, to step Curation: 000D42
- to stream Pmc, to step Checkpoint: 000E00
- to stream Ncbi, to step Merge: 001D35
- to stream Ncbi, to step Curation: 001D35
- to stream Ncbi, to step Checkpoint: 001D35
- to stream Main, to step Merge: 003144
- to stream Main, to step Curation: 003068
Le document en format XML
<record><TEI><teiHeader><fileDesc><titleStmt><title xml:lang="en">Novel Hypoglycemic Dihydropyridones Serendipitously Discovered from O-versus C-Alkylation in The Synthesis of VMAT2 Antagonists</title>
<author><name sortKey="Xie, Yuli" sort="Xie, Yuli" uniqKey="Xie Y" first="Yuli" last="Xie">Yuli Xie</name>
<affiliation wicri:level="1"><nlm:aff id="A1">Department of Medicine of Columbia University Medical Center, New York, NY, 10032, USA</nlm:aff>
<country xml:lang="fr">États-Unis</country>
<wicri:regionArea>Department of Medicine of Columbia University Medical Center, New York, NY, 10032</wicri:regionArea>
<wicri:noRegion>10032</wicri:noRegion>
</affiliation>
</author>
<author><name sortKey="Raffo, Anthony" sort="Raffo, Anthony" uniqKey="Raffo A" first="Anthony" last="Raffo">Anthony Raffo</name>
<affiliation wicri:level="1"><nlm:aff id="A1">Department of Medicine of Columbia University Medical Center, New York, NY, 10032, USA</nlm:aff>
<country xml:lang="fr">États-Unis</country>
<wicri:regionArea>Department of Medicine of Columbia University Medical Center, New York, NY, 10032</wicri:regionArea>
<wicri:noRegion>10032</wicri:noRegion>
</affiliation>
</author>
<author><name sortKey="Ichise, Masanori" sort="Ichise, Masanori" uniqKey="Ichise M" first="Masanori" last="Ichise">Masanori Ichise</name>
<affiliation wicri:level="1"><nlm:aff id="A2">Department of Radiology of Columbia University Medical Center, New York, NY, 10032, USA</nlm:aff>
<country xml:lang="fr">États-Unis</country>
<wicri:regionArea>Department of Radiology of Columbia University Medical Center, New York, NY, 10032</wicri:regionArea>
<wicri:noRegion>10032</wicri:noRegion>
</affiliation>
</author>
<author><name sortKey="Deng, Shixian" sort="Deng, Shixian" uniqKey="Deng S" first="Shixian" last="Deng">Shixian Deng</name>
<affiliation wicri:level="1"><nlm:aff id="A1">Department of Medicine of Columbia University Medical Center, New York, NY, 10032, USA</nlm:aff>
<country xml:lang="fr">États-Unis</country>
<wicri:regionArea>Department of Medicine of Columbia University Medical Center, New York, NY, 10032</wicri:regionArea>
<wicri:noRegion>10032</wicri:noRegion>
</affiliation>
</author>
<author><name sortKey="Harris, Paul E" sort="Harris, Paul E" uniqKey="Harris P" first="Paul E." last="Harris">Paul E. Harris</name>
<affiliation wicri:level="1"><nlm:aff id="A1">Department of Medicine of Columbia University Medical Center, New York, NY, 10032, USA</nlm:aff>
<country xml:lang="fr">États-Unis</country>
<wicri:regionArea>Department of Medicine of Columbia University Medical Center, New York, NY, 10032</wicri:regionArea>
<wicri:noRegion>10032</wicri:noRegion>
</affiliation>
</author>
<author><name sortKey="Landry, Donald W" sort="Landry, Donald W" uniqKey="Landry D" first="Donald W." last="Landry">Donald W. Landry</name>
<affiliation wicri:level="1"><nlm:aff id="A1">Department of Medicine of Columbia University Medical Center, New York, NY, 10032, USA</nlm:aff>
<country xml:lang="fr">États-Unis</country>
<wicri:regionArea>Department of Medicine of Columbia University Medical Center, New York, NY, 10032</wicri:regionArea>
<wicri:noRegion>10032</wicri:noRegion>
</affiliation>
</author>
</titleStmt>
<publicationStmt><idno type="wicri:source">PMC</idno>
<idno type="pmid">18752945</idno>
<idno type="pmc">3632391</idno>
<idno type="url">http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3632391</idno>
<idno type="RBID">PMC:3632391</idno>
<idno type="doi">10.1016/j.bmcl.2008.07.129</idno>
<date when="2008">2008</date>
<idno type="wicri:Area/Pmc/Corpus">000D42</idno>
<idno type="wicri:explorRef" wicri:stream="Pmc" wicri:step="Corpus" wicri:corpus="PMC">000D42</idno>
<idno type="wicri:Area/Pmc/Curation">000D42</idno>
<idno type="wicri:explorRef" wicri:stream="Pmc" wicri:step="Curation">000D42</idno>
<idno type="wicri:Area/Pmc/Checkpoint">000E00</idno>
<idno type="wicri:explorRef" wicri:stream="Pmc" wicri:step="Checkpoint">000E00</idno>
<idno type="wicri:Area/Ncbi/Merge">001D35</idno>
<idno type="wicri:Area/Ncbi/Curation">001D35</idno>
<idno type="wicri:Area/Ncbi/Checkpoint">001D35</idno>
<idno type="wicri:doubleKey">0960-894X:2008:Xie Y:novel:hypoglycemic:dihydropyridones</idno>
<idno type="wicri:Area/Main/Merge">003144</idno>
<idno type="wicri:Area/Main/Curation">003068</idno>
<idno type="wicri:Area/Main/Exploration">003068</idno>
</publicationStmt>
<sourceDesc><biblStruct><analytic><title xml:lang="en" level="a" type="main">Novel Hypoglycemic Dihydropyridones Serendipitously Discovered from O-versus C-Alkylation in The Synthesis of VMAT2 Antagonists</title>
<author><name sortKey="Xie, Yuli" sort="Xie, Yuli" uniqKey="Xie Y" first="Yuli" last="Xie">Yuli Xie</name>
<affiliation wicri:level="1"><nlm:aff id="A1">Department of Medicine of Columbia University Medical Center, New York, NY, 10032, USA</nlm:aff>
<country xml:lang="fr">États-Unis</country>
<wicri:regionArea>Department of Medicine of Columbia University Medical Center, New York, NY, 10032</wicri:regionArea>
<wicri:noRegion>10032</wicri:noRegion>
</affiliation>
</author>
<author><name sortKey="Raffo, Anthony" sort="Raffo, Anthony" uniqKey="Raffo A" first="Anthony" last="Raffo">Anthony Raffo</name>
<affiliation wicri:level="1"><nlm:aff id="A1">Department of Medicine of Columbia University Medical Center, New York, NY, 10032, USA</nlm:aff>
<country xml:lang="fr">États-Unis</country>
<wicri:regionArea>Department of Medicine of Columbia University Medical Center, New York, NY, 10032</wicri:regionArea>
<wicri:noRegion>10032</wicri:noRegion>
</affiliation>
</author>
<author><name sortKey="Ichise, Masanori" sort="Ichise, Masanori" uniqKey="Ichise M" first="Masanori" last="Ichise">Masanori Ichise</name>
<affiliation wicri:level="1"><nlm:aff id="A2">Department of Radiology of Columbia University Medical Center, New York, NY, 10032, USA</nlm:aff>
<country xml:lang="fr">États-Unis</country>
<wicri:regionArea>Department of Radiology of Columbia University Medical Center, New York, NY, 10032</wicri:regionArea>
<wicri:noRegion>10032</wicri:noRegion>
</affiliation>
</author>
<author><name sortKey="Deng, Shixian" sort="Deng, Shixian" uniqKey="Deng S" first="Shixian" last="Deng">Shixian Deng</name>
<affiliation wicri:level="1"><nlm:aff id="A1">Department of Medicine of Columbia University Medical Center, New York, NY, 10032, USA</nlm:aff>
<country xml:lang="fr">États-Unis</country>
<wicri:regionArea>Department of Medicine of Columbia University Medical Center, New York, NY, 10032</wicri:regionArea>
<wicri:noRegion>10032</wicri:noRegion>
</affiliation>
</author>
<author><name sortKey="Harris, Paul E" sort="Harris, Paul E" uniqKey="Harris P" first="Paul E." last="Harris">Paul E. Harris</name>
<affiliation wicri:level="1"><nlm:aff id="A1">Department of Medicine of Columbia University Medical Center, New York, NY, 10032, USA</nlm:aff>
<country xml:lang="fr">États-Unis</country>
<wicri:regionArea>Department of Medicine of Columbia University Medical Center, New York, NY, 10032</wicri:regionArea>
<wicri:noRegion>10032</wicri:noRegion>
</affiliation>
</author>
<author><name sortKey="Landry, Donald W" sort="Landry, Donald W" uniqKey="Landry D" first="Donald W." last="Landry">Donald W. Landry</name>
<affiliation wicri:level="1"><nlm:aff id="A1">Department of Medicine of Columbia University Medical Center, New York, NY, 10032, USA</nlm:aff>
<country xml:lang="fr">États-Unis</country>
<wicri:regionArea>Department of Medicine of Columbia University Medical Center, New York, NY, 10032</wicri:regionArea>
<wicri:noRegion>10032</wicri:noRegion>
</affiliation>
</author>
</analytic>
<series><title level="j">Bioorganic & medicinal chemistry letters</title>
<idno type="ISSN">0960-894X</idno>
<idno type="eISSN">1464-3405</idno>
<imprint><date when="2008">2008</date>
</imprint>
</series>
</biblStruct>
</sourceDesc>
</fileDesc>
<profileDesc><textClass></textClass>
</profileDesc>
</teiHeader>
<front><div type="abstract" xml:lang="en"><p id="P2">Vesicular monoamine transporter type 2 (VMAT2) is a newly emerging target for both diagnostic and therapeutic applications in diabetes mellitus. In pursuit of novel VMAT2 antagonists, we identified a potent hypoglycemic agent with a novel dihydropyridone scaffold. Several analogs were designed and synthesized. A preliminary structure activity relationship (SARs) showed that the dihydropyridone scaffold is required for the activity.</p>
</div>
</front>
</TEI>
<affiliations><list><country><li>États-Unis</li>
</country>
</list>
<tree><country name="États-Unis"><noRegion><name sortKey="Xie, Yuli" sort="Xie, Yuli" uniqKey="Xie Y" first="Yuli" last="Xie">Yuli Xie</name>
</noRegion>
<name sortKey="Deng, Shixian" sort="Deng, Shixian" uniqKey="Deng S" first="Shixian" last="Deng">Shixian Deng</name>
<name sortKey="Harris, Paul E" sort="Harris, Paul E" uniqKey="Harris P" first="Paul E." last="Harris">Paul E. Harris</name>
<name sortKey="Ichise, Masanori" sort="Ichise, Masanori" uniqKey="Ichise M" first="Masanori" last="Ichise">Masanori Ichise</name>
<name sortKey="Landry, Donald W" sort="Landry, Donald W" uniqKey="Landry D" first="Donald W." last="Landry">Donald W. Landry</name>
<name sortKey="Raffo, Anthony" sort="Raffo, Anthony" uniqKey="Raffo A" first="Anthony" last="Raffo">Anthony Raffo</name>
</country>
</tree>
</affiliations>
</record>
Pour manipuler ce document sous Unix (Dilib)
EXPLOR_STEP=$WICRI_ROOT/Sante/explor/SrasV1/Data/Main/Exploration
HfdSelect -h $EXPLOR_STEP/biblio.hfd -nk 003068 | SxmlIndent | more
Ou
HfdSelect -h $EXPLOR_AREA/Data/Main/Exploration/biblio.hfd -nk 003068 | SxmlIndent | more
Pour mettre un lien sur cette page dans le réseau Wicri
{{Explor lien |wiki= Sante |area= SrasV1 |flux= Main |étape= Exploration |type= RBID |clé= PMC:3632391 |texte= Novel Hypoglycemic Dihydropyridones Serendipitously Discovered from O-versus C-Alkylation in The Synthesis of VMAT2 Antagonists }}
Pour générer des pages wiki
HfdIndexSelect -h $EXPLOR_AREA/Data/Main/Exploration/RBID.i -Sk "pubmed:18752945" \ | HfdSelect -Kh $EXPLOR_AREA/Data/Main/Exploration/biblio.hfd \ | NlmPubMed2Wicri -a SrasV1
![]() | This area was generated with Dilib version V0.6.33. | ![]() |