Bridged 5, 6, 7, 8??Tetrahydro??1, 6??naphthyridines, Analogues of Huperzine A: Synthesis, Modelling Studies and Evaluation as Inhibitors of Acetylcholinesterase

…, M De Maeyer, F Compernolle

Index: Vanlaer, Sofie; Voet, Arnout; Gielens, Constant; De Maeyer, Marc; Compernolle, Frans European Journal of Organic Chemistry, 2009 , # 5 p. 643 - 654

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Citation Number: 15

Abstract

Abstract Derivatives of 6, 8-bridged 5, 6, 7, 8-tetrahydro-1, 6-naphthyridines, designed as analogues of huperzine A, were synthesised and evaluated as inhibitors of acetylcholinesterase. In a first approach, C 3-bridged naphthyridines were constructed by internal nucleophilic aromatic substitution of 2-chloro-3-(1-piperidinylmethyl) pyridine precursors containing a 3-CO 2 Me group on the 1-piperidinyl ring moiety. Alternatively, ...