Chemical Sciences, Wyeth Pharmaceuticals, 500 Arcola Road, Collegeville, PA 19426, USA.
Bioorg Med Chem Lett. 2010 Mar 1;20(5):1657-60. doi: 10.1016/j.bmcl.2010.01.073. Epub 2010 Jan 21.
Novel 3-(arylsulfonyl)-1-(azacyclyl)-1H-indoles 6 were synthesized as potential 5-HT(6) receptor ligands, based on constraining a basic side chain as either a piperidine or a pyrrolidine. Many of these compounds had good 5-HT(6) binding affinity with K(i) values <10nM. Depending on substitution, both agonists (e.g., 6o: EC(50)=60nM, E(max)=70%) and antagonists (6y: IC(50)=17 nM, I(max)=86%) were identified in a 5-HT(6) adenylyl cyclase assay.
新型 3-(芳磺酰基)-1-(氮杂环烷基)-1H-吲哚 6 被合成为潜在的 5-HT(6) 受体配体，其基于将碱性侧链约束为哌啶或吡咯烷。这些化合物中有许多具有良好的 5-HT(6) 结合亲和力，Ki 值<10 nM。根据取代基的不同，在 5-HT(6) 腺苷酸环化酶测定中，既鉴定出激动剂（例如 6o：EC(50)=60 nM，E(max)=70%），也鉴定出拮抗剂（6y：IC(50)=17 nM，I(max)=86%）。
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