title: Substituted benzylamino-6-(trifluoromethyl)pyrimidin-4(1H)-ones: a novel class of selective human A-FABP inhibitors.
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.
authors.affiliation: Department of Medicinal Chemistry, Biovitrum AB, SE-751 37 Uppsala, Sweden.
authors.forename: Rune
authors.initials: R
authors.lastname: Ringom
authors.forename: Eva
authors.initials: E
authors.lastname: Axen
authors.forename: Jonas
authors.initials: J
authors.lastname: Uppenberg
authors.forename: Thomas
authors.initials: T
authors.lastname: Lundbäck
authors.forename: Lena
authors.initials: L
authors.lastname: Rondahl
authors.forename: Tjeerd
authors.initials: T
authors.lastname: Barf
mesh_terms: 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
chemical_list: D001596:Benzylamines; D002352:Carrier Proteins; D050556:Fatty Acid-Binding Proteins; D011725:Pyridines; D011743:Pyrimidines; C407065:trifluoromethylpyridine