N,N'-Bisbenzylidenebenzene-1,4-diamines and N,N'-Bisbenzylidenenaphthalene-1,4-diamines as Sirtuin Type 2 (SIRT2) Inhibitors

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• 作者：P&auml ; ivi H. Kiviranta ; Jukka Lepp&auml ; nen ; Sergiy Kyrylenko ; Heikki S. Salo ; Maija Lahtela-Kakkonen ; Anu J. Tervo ; Carsten Wittekindt ; Tiina Suuronen ; Erkki Kuusisto ; Tomi J&auml ; rvinen ; Antero Sal
• 刊名：Journal of Medicinal Chemistry
• 出版年：2006
• 出版时间：December 28, 2006
• 年：2006
• 卷：49
• 期：26
• 页码：7907 - 7911
• 全文大小：59K
• 年卷期：v.49,no.26(December 28, 2006)
• ISSN：1520-4804

文摘

A series of N,N'-bisbenzylidenebenzene-1,4-diamine and N,N'-bisbenzylidenenaphthalene-1,4-diaminederivatives were synthesized as inhibitors for human sirtuin type 2 (SIRT2). The design of the new compoundswas based on two earlier reported hits from molecular modeling and virtual screening. The most potentcompound was N,N'-bis(2-hydroxybenzylidene)benzene-1,4-diamine, which was equipotent with the mostpotent hit compound and well-known SIRT2 inhibitor sirtinol.