S16–1029 is a selective and orally active butyrylcholinesterase ( BChE ) inhibitor with IC 50 s of 11.35 nM and 48.1 nM for eqBChE and hBChE, respectively. S16–1029 could cross the blood-brain barrier (BBB) and reach the central nervous system (CNS). S16–1029 can be used for Alzheimer's disease (AD) research.