Synthesis and structure-activity relationships of 5-substituted pyridine analogues of 3.

@article{Lin2001SynthesisAS,
  title={Synthesis and structure-activity relationships of 5-substituted pyridine analogues of 3.},
  author={N H Lin and Yanfang Li and Yanan He and Mark W. Holladay and T A Kuntzweiler and David J. Anderson and Jeffrey E. Campbell and Stephen Arneric},
  journal={Bioorganic & medicinal chemistry letters},
  year={2001},
  volume={11 5},
  pages={631-3}
}
In an effort to probe the steric influence of C5 substitution of the pyridine ring on CNS binding affinity, analogues of 1 substituted with a bulky moiety--such as phenyl, substituted phenyl, or heteroaryl-were synthesized and tested in vitro for neuronal nicotinic acetylcholine receptor binding affinity. The substituted analogues exhibited Ki values… CONTINUE READING