N,N'-双亚苄基苯-1,4-二胺和N,N'-双亚苄基萘-1,4-二胺作为2型沉默调节蛋白（SIRT2）抑制剂
N,N'-Bisbenzylidenebenzene-1,4-diamines and N,N'-Bisbenzylidenenaphthalene-1,4-diamines as Sirtuin Type 2 (SIRT2) Inhibitors.
作者信息
Kiviranta Päivi H, Leppänen Jukka, Kyrylenko Sergiy, Salo Heikki S, Lahtela-Kakkonen Maija, Tervo Anu J, Wittekindt Carsten, Suuronen Tiina, Kuusisto Erkki, Järvinen Tomi, Salminen Antero, Poso Antti, Wallén Erik A A
机构信息
Department of Pharmaceutical Chemistry , University of Kuopio, P.O. Box 1627, 70211 Kuopio, Finland.
出版信息
J Med Chem. 2006 Dec 28;49(26):7907-11. doi: 10.1021/jm060566j.
A series of N,N'-bisbenzylidenebenzene-1,4-diamine and N,N'-bisbenzylidenenaphthalene-1,4-diamine derivatives were synthesized as inhibitors for human sirtuin type 2 (SIRT2). The design of the new compounds was based on two earlier reported hits from molecular modeling and virtual screening. The most potent compound was N,N'-bis(2-hydroxybenzylidene)benzene-1,4-diamine, which was equipotent with the most potent hit compound and well-known SIRT2 inhibitor sirtinol.
合成了一系列N，N'-双亚苄基苯-1,4-二胺和N，N'-双亚苄基萘-1,4-二胺衍生物作为人2型沉默调节蛋白（SIRT2）的抑制剂。新化合物的设计基于之前通过分子建模和虚拟筛选得到的两个活性化合物。最有效的化合物是N，N'-双（2-羟基亚苄基）苯-1,4-二胺，它与最有效的活性化合物以及著名的SIRT2抑制剂sirtinol具有同等效力。
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