Substituted benzylamino-6-(trifluoromethyl)pyrimidin-4(1 H)-ones: a novel class of selective human A-FABP inhibitors
The synthesis and evaluation of novel human A-FABP inhibitors based on the 6-(trifluoromethyl)pyrimidine-4(1 H)-one scaffold is described. Two series of compounds, bearing either an amino or carbon substituent in the 2-position of the pyrimidine ring were investigated. Modification of substituents a...
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Veröffentlicht in: | Bioorganic & medicinal chemistry letters 2004-09, Vol.14 (17), p.4449-4452 |
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Hauptverfasser: | , , , , , |
Format: | Artikel |
Sprache: | eng |
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Zusammenfassung: | The synthesis and evaluation of novel human A-FABP inhibitors based on the 6-(trifluoromethyl)pyrimidine-4(1
H)-one scaffold is described. Two series of compounds, bearing either an amino or carbon substituent in the 2-position of the pyrimidine ring were investigated. Modification of substituents and chain length optimization led to novel compounds with low micromolar activity and good selectivity for human A-FABP.
The synthesis and biological evaluation of novel human A-FABP inhibitors based on the 6-(trifluoromethyl)pyrimidine-4(1
H)-one scaffold is described. Two series of compounds, bearing either an amino or carbon substituent in the 2-position of the pyrimidine ring were investigated. Modification of substituents and chain length optimization led to novel compounds with low micromolar activity and good selectivity for human A-FABP. |
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ISSN: | 0960-894X 1464-3405 |
DOI: | 10.1016/j.bmcl.2004.06.058 |