Title of article
Discovery of potent and orally active tricyclic-based FBPase inhibitors Original Research Article
Author/Authors
Tomoharu Tsukada، نويسنده , , Osamu Kanno، نويسنده , , Takahiro Yamane، نويسنده , , Jun Tanaka، نويسنده , , Taishi Yoshida، نويسنده , , Akira Okuno، نويسنده , , Takeshi Shiiki، نويسنده , , Mizuki Takahashi، نويسنده , , Takahide Nishi، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2010
Pages
6
From page
5346
To page
5351
Abstract
With the aim of exploring the effect of tricyclic-based FBPase inhibitors in cells and in vivo, a series of prodrugs of tricyclic phosphonates was designed and synthesized. Introducing prodrug moieties into tricyclic-based phosphonates led to the discovery of prodrug 15c, which strongly inhibited glucose production in monkey hepatocytes. Furthermore, prodrug 15c lowered blood glucose levels in fasted cynomolgus monkeys.
Keywords
PET deoxygenation , Galactofuranosidase inhibition , 5-Deoxy-d-galactofuranosides , Galactofuranosidase substrates
Journal title
Bioorganic and Medicinal Chemistry
Serial Year
2010
Journal title
Bioorganic and Medicinal Chemistry
Record number
1306735
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