Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10595585 | Bioorganic & Medicinal Chemistry Letters | 2013 | 8 Pages |
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).
Related Topics
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Authors
Anatoly A. Mazurov, David C. Kombo, Srinivasa Akireddy, Srinivasa Murthy, Terry A. Hauser, Kristen G. Jordan, Gregory J. Gatto, Daniel Yohannes,