Exploration of ring size in a series of cyclic vicinal diamines with σ 1 receptor affinity

…, SD Banister, M Manoli, MR Doddareddy, J Cui…

Index: Moussa, Iman A.; Banister, Samuel D.; Manoli, Miral; Doddareddy, Munikumar Reddy; Cui, Jinquan; MacH, Robert H.; Kassiou, Michael Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 17 p. 5493 - 5497

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Citation Number: 6

Abstract

Imidazolidine and 1, 4-diazepane analogs of N-(2-benzofuranyl) methyl-N′-(4- alkoxybenzyl) piperazines were prepared to explore the effect of ring contraction and expansion on σ receptor affinity and subtype selectivity within a series of cyclic diamines. In vitro receptor binding assays revealed that all cyclic vicinal diamines possessed affinity and selectivity for σ1 receptors. The imidazolidines possessed nanomolar σ1 affinities (Ki= ...