Design, synthesis, evaluation and QSAR analysis of N1-substituted norcymserine derivatives as selective butyrylcholinesterase inhibitors

Abstract

We synthesized a series of N 1-substituted norcymserine derivatives 7a– p and evaluated their anti-cholinesterase activities. In vitro evaluation showed that the pyridinylethyl derivatives 7m– o and the piperidinylethyl derivative 7p improved the anti-butyrylcholinesterase activity by approximately threefold compared to N 1-phenethylnorcymserine (PEC, 2). A quantitative structure-activity relationship (QSAR) study indicated that log S might be a key feature of the improved compounds.