Novel Hypoglycemic Dihydropyridones Serendipitously Discovered from O-versus C-Alkylation in The Synthesis of VMAT2 Antagonists
Identifieur interne : 003144 ( Main/Merge ); précédent : 003143; suivant : 003145Novel 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
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<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>
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