Discovery of highly potent and selective α4β2-nicotinic acetylcholine receptor (nAChR) partial agonists containing an isoxazolylpyridine ether scaffold that …

…, D Brunner, RJ Lukas, AP Kozikowski

Index: Yu, Li-Fang; Eaton, J. Brek; Fedolak, Allison; Zhang, Han-Kun; Hanania, Taleen; Brunner, Dani; Lukas, Ronald J.; Kozikowski, Alan P. Journal of Medicinal Chemistry, 2012 , vol. 55, # 22 p. 9998 - 10009

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Citation Number: 12

Abstract

In our continued efforts to develop α4β2-nicotinic acetylcholine receptor (nAChR) partial agonists as novel antidepressants having a unique mechanism of action, structure–activity relationship (SAR) exploration of certain isoxazolylpyridine ethers is presented. In particular, modifications to both the azetidine ring present in the starting structure 4 and its metabolically liable hydroxyl side chain substituent have been explored to improve ...