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. doi: 10.1016/j.bmcl.2004.06.058.

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

  • Adipocytes / metabolism*
  • Benzylamines / chemistry*
  • Benzylamines / metabolism
  • Benzylamines / pharmacology
  • Carrier Proteins / antagonists & inhibitors*
  • Carrier Proteins / metabolism*
  • Fatty Acid-Binding Proteins
  • Humans
  • Pyridines / chemistry*
  • Pyridines / metabolism
  • Pyridines / pharmacology
  • Pyrimidines / chemistry
  • Pyrimidines / metabolism
  • Pyrimidines / pharmacology

Substances

  • Benzylamines
  • Carrier Proteins
  • Fatty Acid-Binding Proteins
  • Pyridines
  • Pyrimidines
  • trifluoromethylpyridine