Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 18, Issue 18, Pages 5111-5114Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2008.07.129
Keywords
VMAT2; hypoglycemic; SARs; dihydropyridone
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Funding
- PHS
- NIH
- NIDDK [2 RO1 DK63567-05]
- Columbia University DERC [5 P30 DK063608-05]
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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 (SAR) showed that the dihydropyridone scaffold is required for the activity. (C) 2008 Elsevier Ltd. All rights reserved.
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