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2-Arylazetidines as ligands for nicotinic acetylcholine receptors

2-Arylazetidines as ligands for nicotinic acetylcholine receptors

Degennaro, Leonardo, Zenzola, Marina, Laurino, Annunziatina, Cavalluzzi, Maria Maddalena, Franchini, Carlo, Habtemariam, Solomon, Matucci, Rosanna, Luisi, Renzo and Lentini, Giovanni (2017) 2-Arylazetidines as ligands for nicotinic acetylcholine receptors. Chemistry of Heterocyclic Compounds, 53 (3). pp. 329-334. ISSN 0009-3122 (Print), 1573-8353 (Online) (doi:10.1007/s10593-017-2061-5)

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Abstract

Alternative and complementary procedures were adopted for preparing 2-arylazetidine derivatives in moderate to good yields. Preliminary biological evaluation of 2-arylazetidines as ligands of nicotinic acetylcholine receptors allowed to identify chloro-substituted analogs as the most interesting congeners. The title compounds may be considered as suitable hit compounds for developing new nicotinic acetylcholine receptor ligands that may be safer than the currently available drugs targeting nicotinic acetylcholine receptors. Our described synthetic approaches enable facile access to a large number of diversely decorated azetidines for studying the structure–activity relationships and for refining the toxico-pharmacological profile of these agents.

Item Type: Article
Uncontrolled Keywords: azetidine; ligand efficiency metrics; lipophilicity; neurodegeneration; nicotinic acetylcholine receptors; pain; schizophrenia; smoking cessation
Subjects: Q Science > QD Chemistry
Faculty / Department / Research Group: Faculty of Engineering & Science
Faculty of Engineering & Science > Department of Pharmaceutical, Chemical & Environmental Sciences
Last Modified: 06 Apr 2018 16:32
Selected for GREAT 2016: None
Selected for GREAT 2017: None
Selected for GREAT 2018: None
URI: http://gala.gre.ac.uk/id/eprint/19685

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