Development of selective agonists or antagonists for the nicotinic acetylcholine receptors (nAChR) can result in new and potentially useful therapeutic agents. It has been reported in the literature that potent and selective nAChR antagonists might be used for the treatment of nicotine dependence and may be efficacious as therapeutic adjuvants in many different oncologic protocols. We have now designed and synthesized a new series of aminoethers bincorporating a quinuclidine (1a-h) or tropine (2a-h) bicycle and a 4-alkyloxybenzyl moiety. The inhibitory activity of these compounds was determined vs. a7 nAChRs expressed on interneurons in rat hippocampus CA1 slices using the whole-cell patch-clamp. Compounds 1a-h and 2a-h inhibited choline-induced whole-cell currents at low micromolar concentrations (Figure1).The design, synthesis, bioassay and docking studies of these new compounds are presented.

Synthesis, evaluation, and docking of new 4-alkoxybenzyl bicyclic amine ethers as nicotinic acetylcholine receptor antagonists

248th National Meeting (2014)

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