Discovery of novel 2-(4-aryl-2-methylpiperazin-1-yl)-pyrimidin-4-ones as glycogen synthase kinase-3β inhibitors was written by Kohara, Toshiyuki;Nakayama, Kazuki;Watanabe, Kazutoshi;Kusaka, Shin-ichi;Sakai, Daiki;Tanaka, Hiroshi;Fukunaga, Kenji;Sunada, Shinji;Nabeno, Mika;Saito, Ken-ichi;Eguchi, Jun-ichi;Mori, Akiko;Tanaka, Shinji;Bessho, Tomoko;Takiguchi-Hayashi, Keiko;Horikawa, Takashi. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2017.SDS of cas: 147081-29-6 This article mentions the following:
The authors herein describe the results of further evolution of glycogen synthase kinase (GSK)-3β inhibitors from the authors’ promising compounds containing a 3-methylmorpholine moiety. Transformation of the morpholine moiety into a piperazine moiety resulted in potent GSK-3β inhibitors. SAR studies focused on the nitrogen atom of the piperazine moiety revealed that a Ph group afforded potent inhibitory activity toward GSK-3β. Docking studies indicated that the Ph group on the piperazine nitrogen atom and the Me group on the piperazine make cation-π and CH-π interactions with GSK-3β resp. 4-Methoxyphenyl analog 29 (I) showed most potent inhibitory activity toward GSK-3β with good in vitro and in vivo pharmacokinetic profiles, and 29 demonstrated a significant decrease in tau phosphorylation after oral administration in mice. In the experiment, the researchers used many compounds, for example, (S)-tert-Butyl 3-methylpiperazine-1-carboxylate (cas: 147081-29-6SDS of cas: 147081-29-6).
(S)-tert-Butyl 3-methylpiperazine-1-carboxylate (cas: 147081-29-6) belongs to piperazine derivatives. Piperazine causes primary dermal irritation and skin burns at high concentrations. Piperazine also causes eye irritation in humans. Outside the body, piperazine has a remarkable power to dissolve uric acid and producing a soluble urate, but in clinical experience it has not proved equally successful. SDS of cas: 147081-29-6
Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics