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  • Design, synthesis, evaluation and QSAR analysis of N(1)-substituted norcymserine derivatives as selective butyrylcholinesterase inhibitors.

Design, synthesis, evaluation and QSAR analysis of N(1)-substituted norcymserine derivatives as selective butyrylcholinesterase inhibitors.

Bioorganic & medicinal chemistry letters (2010-02-09)
Jun Takahashi, Ichiro Hijikuro, Takeshi Kihara, Modachur G Murugesh, Shinichiro Fuse, Ryo Kunimoto, Yoshinori Tsumura, Akinori Akaike, Tetsuhiro Niidome, Yasushi Okuno, Takashi Takahashi, Hachiro Sugimoto
PMID20137934
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 logS might be a key feature of the improved compounds.