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
Hauptverfasser: Ringom, Rune, Axen, Eva, Uppenberg, Jonas, Lundbäck, Thomas, Rondahl, Lena, Barf, Tjeerd
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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.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2004.06.058