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Bioorg Med Chem Lett. 2013 Jul 1;23(13):3927-34. doi: 10.1016/j.bmcl.2013.04.058. Epub 2013 May 1.

Novel nicotinic acetylcholine receptor agonists containing carbonyl moiety as a hydrogen bond acceptor.

Author information

1
Targacept, Inc., 100 North Main Street, Winston-Salem, NC 27101, USA. galana99@yahoo.com

Abstract

A novel series of α4β2 nAChR agonists lacking common pyridine or its bioisosteric heterocycle have been disclosed. Essential pharmacophoric elements of the series are exocyclic carbonyl moiety as a hydrogen bond acceptor and secondary amino group within diaza- or azabicyclic scaffold. Computer modeling studies suggested that molecular shape of the ligand also contributes to promotion of agonism. Proof of concept for improving working memory performance in a novel object recognition task has been demonstrated on a representative of the series, 3-propionyl-3,7-diazabicyclo[3.3.0]octane (34).

PMID:
23692872
DOI:
10.1016/j.bmcl.2013.04.058
[Indexed for MEDLINE]

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