Novel aryl and heteroaryl substituted N-[3-(4-phenylpiperazin-1-yl) propyl]-1, 2, 4-oxadiazole-5-carboxamides as selective GSK-3 inhibitors

…, EA Katrukha, VI Kazey, I Okun, DV Kravchenko…

Index: 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. Bioorganic and Medicinal Chemistry Letters, 2008 , vol. 18, # 12 p. 3661 - 3666

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Citation Number: 24

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-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 ...