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<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><nlm:aff id="A1">Department of Medicine of Columbia University Medical Center, New York, NY, 10032, USA</nlm:aff></affiliation></author><author><name sortKey="Raffo, Anthony" sort="Raffo, Anthony" uniqKey="Raffo A" first="Anthony" last="Raffo">Anthony Raffo</name><affiliation><nlm:aff id="A1">Department of Medicine of Columbia University Medical Center, New York, NY, 10032, USA</nlm:aff></affiliation></author><author><name sortKey="Ichise, Masanori" sort="Ichise, Masanori" uniqKey="Ichise M" first="Masanori" last="Ichise">Masanori Ichise</name><affiliation><nlm:aff id="A2">Department of Radiology of Columbia University Medical Center, New York, NY, 10032, USA</nlm:aff></affiliation></author><author><name sortKey="Deng, Shixian" sort="Deng, Shixian" uniqKey="Deng S" first="Shixian" last="Deng">Shixian Deng</name><affiliation><nlm:aff id="A1">Department of Medicine of Columbia University Medical Center, New York, NY, 10032, USA</nlm:aff></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><nlm:aff id="A1">Department of Medicine of Columbia University Medical Center, New York, NY, 10032, USA</nlm:aff></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><nlm:aff id="A1">Department of Medicine of Columbia University Medical Center, New York, NY, 10032, USA</nlm:aff></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></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><nlm:aff id="A1">Department of Medicine of Columbia University Medical Center, New York, NY, 10032, USA</nlm:aff></affiliation></author><author><name sortKey="Raffo, Anthony" sort="Raffo, Anthony" uniqKey="Raffo A" first="Anthony" last="Raffo">Anthony Raffo</name><affiliation><nlm:aff id="A1">Department of Medicine of Columbia University Medical Center, New York, NY, 10032, USA</nlm:aff></affiliation></author><author><name sortKey="Ichise, Masanori" sort="Ichise, Masanori" uniqKey="Ichise M" first="Masanori" last="Ichise">Masanori Ichise</name><affiliation><nlm:aff id="A2">Department of Radiology of Columbia University Medical Center, New York, NY, 10032, USA</nlm:aff></affiliation></author><author><name sortKey="Deng, Shixian" sort="Deng, Shixian" uniqKey="Deng S" first="Shixian" last="Deng">Shixian Deng</name><affiliation><nlm:aff id="A1">Department of Medicine of Columbia University Medical Center, New York, NY, 10032, USA</nlm:aff></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><nlm:aff id="A1">Department of Medicine of Columbia University Medical Center, New York, NY, 10032, USA</nlm:aff></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><nlm:aff id="A1">Department of Medicine of Columbia University Medical Center, New York, NY, 10032, USA</nlm:aff></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><pmc article-type="research-article"><pmc-comment>The publisher of this article does not allow downloading of the full text in XML form.</pmc-comment>
<pmc-dir>properties manuscript</pmc-dir>
<front><journal-meta><journal-id journal-id-type="nlm-journal-id">9107377</journal-id><journal-id journal-id-type="pubmed-jr-id">20409</journal-id><journal-id journal-id-type="nlm-ta">Bioorg Med Chem Lett</journal-id><journal-id journal-id-type="iso-abbrev">Bioorg. Med. Chem. Lett.</journal-id><journal-title-group><journal-title>Bioorganic & medicinal chemistry letters</journal-title></journal-title-group><issn pub-type="ppub">0960-894X</issn><issn pub-type="epub">1464-3405</issn></journal-meta><article-meta><article-id pub-id-type="pmid">18752945</article-id><article-id pub-id-type="pmc">3632391</article-id><article-id pub-id-type="doi">10.1016/j.bmcl.2008.07.129</article-id><article-id pub-id-type="manuscript">NIHMS70436</article-id><article-categories><subj-group subj-group-type="heading"><subject>Article</subject></subj-group></article-categories><title-group><article-title>Novel Hypoglycemic Dihydropyridones Serendipitously Discovered from O-versus C-Alkylation in The Synthesis of VMAT2 Antagonists</article-title></title-group><contrib-group><contrib contrib-type="author"><name><surname>Xie</surname><given-names>Yuli</given-names></name><xref ref-type="aff" rid="A1">a</xref></contrib><contrib contrib-type="author"><name><surname>Raffo</surname><given-names>Anthony</given-names></name><xref ref-type="aff" rid="A1">a</xref></contrib><contrib contrib-type="author"><name><surname>Ichise</surname><given-names>Masanori</given-names></name><xref ref-type="aff" rid="A2">b</xref></contrib><contrib contrib-type="author"><name><surname>Deng</surname><given-names>Shixian</given-names></name><xref ref-type="aff" rid="A1">a</xref></contrib><contrib contrib-type="author"><name><surname>Harris</surname><given-names>Paul E.</given-names></name><xref ref-type="aff" rid="A1">a</xref></contrib><contrib contrib-type="author"><name><surname>Landry</surname><given-names>Donald W.</given-names></name><xref ref-type="aff" rid="A1">a</xref><xref rid="FN1" ref-type="author-notes">*</xref></contrib></contrib-group><aff id="A1"><label>a</label>Department of Medicine of Columbia University Medical Center, New York, NY, 10032, USA</aff><aff id="A2"><label>b</label>Department of Radiology of Columbia University Medical Center, New York, NY, 10032, USA</aff><author-notes><corresp id="FN1"><label>*</label>Corresponding author. Tel: +1 212 3055839; Fax: +1 212 3053475; <email>dwl1@columbia.edu</email></corresp></author-notes><pub-date pub-type="nihms-submitted"><day>3</day><month>4</month><year>2013</year></pub-date><pub-date pub-type="epub"><day>07</day><month>8</month><year>2008</year></pub-date><pub-date pub-type="ppub"><day>15</day><month>9</month><year>2008</year></pub-date><pub-date pub-type="pmc-release"><day>22</day><month>4</month><year>2013</year></pub-date><volume>18</volume><issue>18</issue><fpage>5111</fpage><lpage>5114</lpage><permissions><copyright-statement>© 2008 Elsevier Ltd. All rights reserved.</copyright-statement><copyright-year>2008</copyright-year></permissions><abstract><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></abstract><kwd-group><kwd>VMAT2</kwd><kwd>hypoglycemic</kwd><kwd>SARs</kwd><kwd>dihydropyridone</kwd></kwd-group><funding-group><award-group><funding-source country="United States">National Institute of Diabetes and Digestive and Kidney Diseases : NIDDK</funding-source><award-id>R01 DK077493 || DK</award-id></award-group><award-group><funding-source country="United States">National Institute of Diabetes and Digestive and Kidney Diseases : NIDDK</funding-source><award-id>R01 DK063567 || DK</award-id></award-group></funding-group></article-meta></front></pmc></record>Pour manipuler ce document sous Unix (Dilib)
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