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Spiro[pyrrolidine-3,3′-oxindoles] as 5-HT7 receptor ligands
Bioorganic & Medicinal Chemistry Letters ( IF 2.5 ) Pub Date : 2018-06-12 , DOI: 10.1016/j.bmcl.2018.06.019
Ádám Andor Kelemen , Grzegorz Satała , Andrzej J. Bojarski , György M. Keserű

Here we report the design and synthesis of spiro[pyrrolidine-3,3′-oxindole] derivatives representing a novel scaffold of 5-HT7 receptor ligands. The synthesized analogues were validated as low nanomolar ligands showing selectivity in a panel of related serotonin receptor subtypes including 5-HT1AR, 5-HT2AR and 5-HT6R.



中文翻译:

螺[吡咯烷-3,3'-羟吲哚]作为5-HT 7受体配体

在这里,我们报告设计和合成的螺[吡咯烷-3,3'-oxindole]衍生物代表5-HT 7受体配体的新型支架。合成的类似物被验证为低纳摩尔配体,在一系列相关的5-羟色胺受体亚型(包括5-HT 1A R,5-HT 2A R和5-HT 6 R)中显示出选择性。

更新日期:2018-06-12
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