Syntheses and structure-activity relationship (SAR) studies of 2,5-diazabicyclo[2.2.1]heptanes as novel alpha7 neuronal nicotinic receptor (NNR) ligands

Biaryl substituted 2,5-diazabicyclo[2.2.1]heptanes have been synthesized and tested for their affinity toward alpha7 neuronal nicotinic receptors (NNRs). SAR studies established that 5-N-methyl substituent, heteroaryl linker and the nature of terminal aryl group are critical for the ligand to achiev...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2010-06, Vol.20 (12), p.3636-3639
Main Authors: Li, Tao, Bunnelle, William H, Ryther, Keith B, Anderson, David J, Malysz, John, Helfrich, Rosalind, Grønlien, Jens H, Håkerud, Monika, Peters, Dan, Schrimpf, Michael R, Gopalakrishnan, Murali, Ji, Jianguo
Format: Article
Language:English
Subjects:
Animals
Heptanes - chemical synthesis
Heptanes - chemistry
Heptanes - pharmacology
Humans
Ligands
Neurons - metabolism
Nicotinic Agonists - chemical synthesis
Nicotinic Agonists - chemistry
Protein Binding
Radioligand Assay
Rats
Receptors, Nicotinic - drug effects
Receptors, Nicotinic - metabolism
Structure-Activity Relationship
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Summary:Biaryl substituted 2,5-diazabicyclo[2.2.1]heptanes have been synthesized and tested for their affinity toward alpha7 neuronal nicotinic receptors (NNRs). SAR studies established that 5-N-methyl substituent, heteroaryl linker and the nature of terminal aryl group are critical for the ligand to achieve potent alpha7 NNR agonist activity.
ISSN:1464-3405
DOI:10.1016/j.bmcl.2010.04.105