- FLUORO-[1,3]OXAZINES AS BACE1 INHIBITORS
-
The present invention provides a compound of formula I having BACE1 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are u
- -
-
Page/Page column 41; 46-47
(2016/02/28)
-
- Novel aryl and heteroaryl substituted N-[3-(4-phenylpiperazin-1-yl)propyl]-1,2,4-oxadiazole-5-carboxamides as selective GSK-3 inhibitors
-
Synthesis, biological evaluation, and SAR dependencies for a series of novel aryl and heteroaryl substituted N-[3-(4-phenylpiperazin-1-yl)propyl]-1,2,4-oxadiazole-5-carboxamide inhibitors of GSK-3β kinase are described. The inhibitory activity of the synthesized compounds is highly dependent on the character of substituents in the phenyl ring and the nature of terminal heterocyclic fragment of the core molecular scaffold. The most potent compounds from this series contain 3,4-di-methyl or 2-methoxy substituents within the phenyl ring and 3-pyridine fragment connected to the 1,2,4-oxadiazole heterocycle. These compounds selectively inhibit GSK-3β kinase with IC50 value of 0.35 and 0.41 μM, respectively.
- Koryakova, Angela G.,Ivanenkov, Yan A.,Ryzhova, Elena A.,Bulanova, Elena A.,Karapetian, Ruben N.,Mikitas, Olga V.,Katrukha, Eugeny A.,Kazey, Vasily I.,Okun, Ilya,Kravchenko, Dmitry V.,Lavrovsky, Yan V.,Korzinov, Oleg M.,Ivachtchenko, Alexandre V.
-
supporting information; experimental part
p. 3661 - 3666
(2009/04/16)
-