Substituted benzylamino-6-(trifluoromethyl)pyrimidin-4(1H)-ones: a novel class of selective human A-FABP inhibitors.

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Ringom R, Axen E, Uppenberg J, Lundback T, Rondahl L, Barf T

Substituted benzylamino-6-(trifluoromethyl)pyrimidin-4(1H)-ones: a novel class of selective human A-FABP inhibitors.

Bioorg Med Chem Lett. 2004 Sep 6;14(17):4449-52.

PubMed ID

15357970 [ View in PubMed

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Abstract

The synthesis and biological evaluation of novel human A-FABP inhibitors based on the 6-(trifluoromethyl)pyrimidine-4(1H)-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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Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
2-{[2-Oxo-2-(1-piperidinyl)ethyl]sulfanyl}-6-(trifluoromethyl)-4(1H)-pyrimidinone	Fatty acid-binding protein, adipocyte	IC 50 (nM)	1000	N/A	N/A	Details