Abstract
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.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Acetylation
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Binding Sites
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Diamines / chemical synthesis
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Diamines / chemistry
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Diamines / pharmacology*
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Humans
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Molecular Structure
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Phenylenediamines / chemical synthesis
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Phenylenediamines / chemistry
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Phenylenediamines / pharmacology*
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Sirtuin 2
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Sirtuins / antagonists & inhibitors*
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Sirtuins / metabolism
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Structure-Activity Relationship
Substances
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Diamines
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N,N'-bis(2-hydroxybenzylidene)benzene-1,4-diamine
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Phenylenediamines
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SIRT2 protein, human
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Sirtuin 2
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Sirtuins