Substituted benzylamino-6-(trifluoromethyl)pyrimidin-4(1H)-ones: a novel class of selective human A-FABP inhibitors.
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.
Ringom
Rune
R
Department of Medicinal Chemistry, Biovitrum AB, SE-751 37 Uppsala, Sweden.
Axen
Eva
E
Uppenberg
Jonas
J
Lundbäck
Thomas
T
Rondahl
Lena
L
Barf
Tjeerd
T
D017667:Adipocytes / Q000378:metabolism*; D001596:Benzylamines / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology; D002352:Carrier Proteins / Q000037:antagonists & inhibitors* / Q000378:metabolism*; D050556:Fatty Acid-Binding Proteins; D006801:Humans; D011725:Pyridines / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology; D011743:Pyrimidines / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology
D001596:Benzylamines; D002352:Carrier Proteins; D050556:Fatty Acid-Binding Proteins; D011725:Pyridines; D011743:Pyrimidines; C407065:trifluoromethylpyridine