3-Aryl-3-arylmethoxyazetidines. A new class of high affinity ligands for monoamine transporters

A Thaxton, S Izenwasser, D Wade, ED Stevens…

Index: Thaxton, Amber; Izenwasser, Sari; Wade, Dean; Stevens, Edwin D.; Mobley, David L.; Jaber, Vivian; Lomenzo, Stacey A.; Trudell, Mark L. Bioorganic and Medicinal Chemistry Letters, 2013 , vol. 23, # 15 p. 4404 - 4407

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Abstract

A series of 3-aryl-3-arylmethoxy-azetidines were synthesized and evaluated for binding affinities at dopamine and serotonin transporters. The 3-aryl-3-arylmethoxyazetidines were generally SERT selective with the dichloro substituted congener 7c (Ki= 1.0 nM) and the tetrachloro substituted derivative 7i (Ki= 1.3 nM) possessing low nanomolar affinity for the SERT. The 3-(3, 4-dichlorophenyl-3-phenylmethoxyazetidine (7g) exhibited moderate ...