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.
MeSH terms
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Adipocytes / metabolism*
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Benzylamines / chemistry*
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Benzylamines / metabolism
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Benzylamines / pharmacology
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Carrier Proteins / antagonists & inhibitors*
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Carrier Proteins / metabolism*
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Fatty Acid-Binding Proteins
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Humans
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Pyridines / chemistry*
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Pyridines / metabolism
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Pyridines / pharmacology
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Pyrimidines / chemistry
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Pyrimidines / metabolism
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Pyrimidines / pharmacology
Substances
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Benzylamines
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Carrier Proteins
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Fatty Acid-Binding Proteins
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Pyridines
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Pyrimidines
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trifluoromethylpyridine