4- Substituted sampangine derivatives: Novel acetylcholinesterase and β-myloid aggregation inhibitors.

A series of 4- substituted sampangine derivatives (4-aminoalkylaminosampangine Ar-NH(CH)NRR) has been designed, synthesized, and tested for their ability to inhibit acetylcholinesterase (AChE), butyrylcholinesterase (BChE) and β-myloid (Aβ) aggregation. The synthetic compounds exhibited high AChE inhibitory activity and a significant in vitro inhibitory potency toward the self-induced Aβ aggregation. While, treatment of SH-SY5Y cells overexpressing the Swedish mutant form of human β-amyloid precursor protein (APPsw) with derivatives was associated with significant reduction of Aβ42 secretion levels.