LITEBAMINE N-HOMOLOGS - PREPARATION AND ANTIACETYLCHOLINESTERASE ACTIVITY

Litebamine N-homologues were easily prepared from laurolitsine, genera lly via three reaction steps (N-alkylation, solvolysis with 1 M NH4OAc under reflux, and the Mannich reaction) in more than 80% overall yiel d. Among the prepared compounds, N-propyl-, N-isobutyl-, and N-isoprop ylnorlitebamines exhibited moderate antiacetylcholinesterase activity (IC50 Ca 7.0 mu M), while the corresponding N-metho salt of N-propylno rlitebamine showed potent activity (IC50 2.70 mu M).