1132814-48-2Relevant academic research and scientific papers
Quinolone derivatives containing strained spirocycle as orally active glycogen synthase kinase 3β (GSK-3β) inhibitors for type 2 diabetics
Seto, Shigeki,Yumoto, Kazuhiko,Okada, Kyoko,Asahina, Yoshikazu,Iwane, Aya,Iwago, Maki,Terasawa, Reiko,Shreder, Kevin R.,Murakami, Koji,Kohno, Yasushi
, p. 1188 - 1200 (2012/03/26)
The design, synthesis, and evaluation of 6-6-7 tricyclic quinolones containing the strained spirocycle moiety aiming at the GSK-3β inhibitor were described. Among the synthesized compounds, 44, having a cyclobutane ring on a spirocycle, showed excellent GSK-3β inhibitory activity in both cell-free and cell-based assays (IC50 = 36 nM, EC50 = 3.2 μM, respectively). Additionally, 44 decreased the plasma glucose concentration dose-dependently after an oral glucose tolerance test in mice.
Synthesis and structural analysis of a new class of azaspiro[3.3]heptanes as building blocks for medicinal chemistry
Burkhard, Johannes A.,Guerot, Carine,Knust, Henner,Rogers-Evans, Mark,Carreira, Erick M.
supporting information; experimental part, p. 1944 - 1947 (2010/07/04)
Figure presented Straightforward access toward previously unreported substituted, heterocyclic spiro[3.3]heptanes is disclosed. These spirocyclic systems may be considered as alternatives to 1,3-heteroatom-substituted cyclohexanes, which are otherwise insufficiently stable to allow their use in drug discovery. Conformational details are discussed on the basis of X-ray crystallographic structures.
SPIROCYCLIC AMINOQUINOLONES AS GSK-3 INHIBITORS
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Page/Page column 107-108, (2009/04/25)
Provided herein are spirocyclic aminoquinolones of formula I and compositions containing the compounds. The compounds and compositions provided herein are useful in the prevention, amelioration or treatment of GSK- 3 inhibitors mediated diseases. In Formu
