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ID: ALA2407030
Journal: Bioorg Med Chem Lett
Title: Novel nicotinic acetylcholine receptor agonists containing carbonyl moiety as a hydrogen bond acceptor.
Authors: Mazurov AA, Kombo DC, Akireddy S, Murthy S, Hauser TA, Jordan KG, Gatto GJ, Yohannes D.
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).
CiteXplore: 23692872