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. 2018 Aug 1;28(14):2418-2421.
doi: 10.1016/j.bmcl.2018.06.019. Epub 2018 Jun 12.

Spiro[pyrrolidine-3,3'-oxindoles] as 5-HT 7 Receptor Ligands

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Spiro[pyrrolidine-3,3'-oxindoles] as 5-HT 7 Receptor Ligands

Ádám Andor Kelemen et al. Bioorg Med Chem Lett. .

Abstract

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.

Keywords: 5-HT(7)R; G-protein coupled receptor; Oxidative spiro-rearrangement; Oxindole; Pharmacophore model.

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