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

AA Mazurov, DC Kombo, S Akireddy, S Murthy…

Index: Mazurov, Anatoly A.; Kombo, David C.; Akireddy, Srinivasa; Murthy, Srinivasa; Hauser, Terry A.; Jordan, Kristen G.; Gatto, Gregory J.; Yohannes, Daniel Bioorganic and Medicinal Chemistry Letters, 2013 , vol. 23, # 13 p. 3927 - 3934

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Citation Number: 9

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 ...