1361253-37-3Relevant articles and documents
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
experimental part, 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.
