Eur J Med Chem 2021 Mar 15;218:113385. Epub 2021 Mar 15.
Department of Environmental Health Sciences, University of Michigan, Ann Arbor, MI, 48109, USA; Department of Neurology, University of Michigan, Ann Arbor, MI, 48109, USA; Center of Computational Medicine and Bioinformatics, University of Michigan, Ann Arbor, MI, 48109, USA. Electronic address:
An expanded series of alkyl 2-arylhydrazinylidene-3-oxo-3-polyfluoroalkylpropionates (HOPs) 3 was obtained via Cu(OAc)-catalyzed azo coupling. All were nanomolar inhibitors of carboxylesterase (CES), while moderate or weak inhibitors of acetylcholinesterase and butyrylcholinesterase. Steady-state kinetics studies showed that HOPs 3 are mixed type inhibitors of the three esterases. Read More