Synthesis and biological evaluation of pyridine-modified analogues of 3-(2-aminoethoxy) pyridine as novel nicotinic receptor ligands

…, L Dong, WH Bunnelle, DJ Anderson, MD Meyer

Index: Lin, Nan-Horng; Dong, Liming; Bunnelle, William H; Anderson, David J; Meyer, Michael D Bioorganic and Medicinal Chemistry Letters, 2002 , vol. 12, # 22 p. 3321 - 3324

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Citation Number: 16

Abstract

Analogues of the potent nicotinic receptor agonist 3-(2-aminoethoxy) pyridine substituted at the 5′ and 6′-positions of the pyridine ring were synthesized and tested in vitro for nicotinic receptor binding activity (displacement of [3H](−) cytisine from whole rat brain synaptic membranes). The substituted analogues exhibited Ki values ranging from 0.076 to 319 nM compared to a Ki value of 26 nM for compound 1. Among the compounds tested, 5 ...