Alzheimer’s disease (AD) is a complex neurodegenerative disorder affecting millions of people world-wide. The underlying pathologic mechanisms of AD are unclear. Over the decades, the development of single target agent did not lead to any successful treatment for AD. Multi-target agent that could tackle more than one AD phenotypes may be helpful as a treatment strategy. Cholinesterases (ChEs) including acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE), are currently the drug targets with approved treatments. Moreover, amyloid beta (Aβ) deposition is a hallmark of AD, which receives considerable attention. Herein, 9Q, a previously reported dual target inhibitor dealing with cholinergic dysfunction and amyloid deposition for AD treatment, was undergone thorough investigations. In vitro studies revealed that 9Q exhibited over 80% inhibition on ChEs activity at 100 μM and more than 30% inhibition on Aβ aggregation at 1 mM concentration. Moreover 9Q was able to penetrate the blood brain barrier (BBB) and enhance the cerebral acetylcholine level in triple transgenic AD (3xTg-AD) mice. Following one month treatment with 9Q, the amyloid burden and the cognitive deficits in 3xTg-AD mice were significantly ameliorated. It was observed that 9Q treatment mitigated the synapse dysfunction, decreased the amyloidogenic APP processing and reduced the tau pathology in 3xTg-AD mice. Taken together, our results suggested that dual inhibition of cholinesterases and Aβ aggregation could be a promising approach in AD treatment.