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首页> 外文期刊>Journal of Medicinal Chemistry >iV,iV'-Bisbenzylidenebenzene-l,4-diamines and N,N-Bisbenzylidenenaphthalene-l,4-diamines as Sirtuin Type 2 (SIRT2) Inhibitors
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iV,iV'-Bisbenzylidenebenzene-l,4-diamines and N,N-Bisbenzylidenenaphthalene-l,4-diamines as Sirtuin Type 2 (SIRT2) Inhibitors

机译:iV,iV'-双亚苄基苯-1,4-二胺和N,N-双亚苄基萘-1,4-二胺作为Sirtuin 2型(SIRT2)抑制剂

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摘要

A series of N,N'-bisbenzylidenebenzene-l,4-diamine and N,N'-bisbenzylidenenaphthalene-l,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-l,4-diamine,which was equipotent with the most potent hit compound and well-known SIRT2 inhibitor sirtinol.
机译: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类sirtuin 2型(SIRT2)的抑制剂。分子建模和虚拟筛选中两个较早报道的命中化合物。最有效的化合物是N,N'-双(2-羟基亚苄基)苯-1,4-二胺,与最有效的命中化合物和著名的SIRT2等价抑制剂西地醇。

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