Abstract
A new inhibitor for human sirtuin type proteins 1 and 2 (SIRT1 and SIRT2) was discovered through virtual database screening in search of new scaffolds. A series of compounds was synthesized based on the hit compound (3-[[3-(4-tert-butylphenyl)1,2,4-oxadiazole-5-carbonyl]amino]-1-[3-(trifluoromethyl)phenyl]thiourea). The most potent compound in the series was nearly as potent as the reference compound (6-chloro-2,3,4,9-tetrahydro-1H-carbazole-1-carboxamide).
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Enzyme Inhibitors / chemical synthesis*
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Enzyme Inhibitors / chemistry
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Enzyme Inhibitors / pharmacology*
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Humans
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Models, Molecular
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Molecular Structure
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Oxadiazoles / chemistry*
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Oxadiazoles / pharmacology
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Semicarbazides / chemical synthesis*
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Semicarbazides / chemistry
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Semicarbazides / pharmacology*
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Sirtuin 1
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Sirtuin 2
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Sirtuins / antagonists & inhibitors*
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Sirtuins / chemistry
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Sirtuins / metabolism
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Structure-Activity Relationship
Substances
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Enzyme Inhibitors
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Oxadiazoles
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Semicarbazides
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thiosemicarbazide
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SIRT1 protein, human
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SIRT2 protein, human
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Sirtuin 1
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Sirtuin 2
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Sirtuins