Referenced in: none

Automatically associated channels: TASK1

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

Authors: Anatoly A Mazurov, David C Kombo, Srinivasa Akireddy, Srinivasa Murthy, Terry A Hauser, Kristen G Jordan, Gregory J Gatto, Daniel Yohannes

Journal, date & volume: Bioorg. Med. Chem. Lett., 2013 Jul 1 , 23, 3927-34

PubMed link: http://www.ncbi.nlm.nih.gov/pubmed/23692872

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).