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ID: ALA1145578
Journal: Bioorg Med Chem Lett
Title: Novel aryl and heteroaryl substituted N-[3-(4-phenylpiperazin-1-yl)propyl]-1,2,4-oxadiazole-5-carboxamides as selective GSK-3 inhibitors.
Authors: Koryakova AG, Ivanenkov YA, Ryzhova EA, Bulanova EA, Karapetian RN, Mikitas OV, Katrukha EA, Kazey VI, Okun I, Kravchenko DV, Lavrovsky YV, Korzinov OM, Ivachtchenko AV.
Abstract: 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-3beta 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-3beta kinase with IC(50) value of 0.35 and 0.41 microM, respectively.
CiteXplore: 18502121