Abstract
A series of N-(3-(4-hydroxyphenyl)-propenoyl)-amino acid tryptamides was based on a previously reported new SIRT2 inhibitor from our group, and it was designed to study if the molecular size of the compound could be reduced. The most potent compounds, N-(3-(4-hydroxyphenyl)-propenoyl)-2-aminoisobutyric acid tryptamide and N-(3-(4-hydroxyphenyl)-propenoyl)-L-alanine tryptamide, were equipotent, 30% smaller in molecular weight, and slightly more selective (SIRT2/SIRT1) than the parent compound.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Catalysis
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Chemistry, Pharmaceutical / methods*
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Drug Design
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Humans
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Inhibitory Concentration 50
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Models, Chemical
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Molecular Structure
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Molecular Weight
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Niacinamide / analogs & derivatives*
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Niacinamide / chemical synthesis
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Niacinamide / pharmacology
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Sirtuin 1
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Sirtuin 2
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Sirtuins / antagonists & inhibitors*
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Tryptamines / chemical synthesis*
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Tryptamines / pharmacology*
Substances
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Tryptamines
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Niacinamide
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tryptamide
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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