Alzheimer's disease, which is characterised by reduced cholinergic functioning, is generally treated by acetylcholinesterase inhibitors such as donepezil. Although treatment exists, it remains symptomatic and subject to unfavorable adverse effects. Drug discovery is rife with ineffective, cytotoxic, and/or pharmacokinetically unfeasible pharmacophores. The purpose of this study is to assess novel pharmacophores’ in vitro acetylcholinesterase inhibitory, blood-brain barrier permeability and cytotoxic potential.