Highly Selective Butyrylcholinesterase Inhibitors Related to Amaryllidaceae Alkaloids - Design, Synthesis, and Biological Evaluation

Carltonine-Derived Compounds for Targeted Butyrylcholinesterase Inhibition

“…In our recent studies, we reported the isolation of Amaryllidaceae alkaloids (AAs) and the synthesis of firstin-class compounds possessing promising BChE inhibitory properties. [56][57][58][59] A newly isolated and unique structural framework of AAs referred to as the carltonine-type expanded the chemical space by a new structural scaffold, designated as carltonines A-E. Building upon these findings, our subsequent investigations probe the synthesis of a first series of highly selective BChE inhibitors, shedding light on key aspects of the structureactivity relationship (SAR) pertinent to BChE inhibition. Here, we report the design, synthesis, and biological evaluation of a compound library as a follow-up to carltonine drug discovery, building upon the previously observed SAR.…”