Synthesis and binding assays of novel 3, 3-dimethylpiperidine derivatives with various lipophilicities as σ 1 receptor ligands

…, NA Colabufo, M Contino, R Perrone, F Berardi

文献索引：Ferorelli, Savina; Abate, Carmen; Pedone, Maria P.; Colabufo, Nicola A.; Contino, Marialessandra; Perrone, Roberto; Berardi, Francesco Bioorganic and Medicinal Chemistry, 2011 , vol. 19, # 24 p. 7612 - 7622

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被引用次数: 4

摘要

Starting from two carbocyclic analogs, a series of 3, 3-dimethylpiperidine derivatives was prepared and tested in radioligand binding assays at σ1 and σ2 receptors, and at Δ8–Δ7 sterol isomerase (SI) site. The novel compounds mostly bear heterocyclic rings or bicyclic nucleus of differing lipophilicities. Compounds 18a and 19a, b demonstrated the highest σ1 affinity (Ki= 0.14–0.38 nM) with a good selectivity versus σ2 binding. Among them, 18a ...