163719-80-0Relevant academic research and scientific papers
Some regularities of the synthesis of ethyl 3-aryl-1,2,4-oxadiazole-5-carboxylates
Voronova,Baikov,Krasovskaya,Kolobov,Kofanov
, p. 1683 - 1686 (2015/02/02)
Features of amidoximes reactions with ethyl chlorooxalate in a wide range of solvents at the use of a number of bases were investigated. An efficient preparation method for ethyl 3-aryl-1,2,4-oxadiazole-5-carboxylates in acetonitrile in the presence of triethylamine was developed.
Novel aryl and heteroaryl substituted N-[3-(4-phenylpiperazin-1-yl)propyl]-1,2,4-oxadiazole-5-carboxamides as selective GSK-3 inhibitors
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)
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.
