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Bioorg Med Chem Lett. 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-HT7 receptor ligands.

Author information

1
Medicinal Chemistry Research Group, Research Centre for Natural Sciences, Hungarian Academy of Sciences, Magyar tudósok körútja 2, H3660, 23-3650, 96, 1117 Budapest, Hungary.
2
Department of Medicinal Chemistry, Institute of Pharmacology, Polish Academy of Sciences, 12 Smętna Street, 31-343 Krakow, Poland.
3
Medicinal Chemistry Research Group, Research Centre for Natural Sciences, Hungarian Academy of Sciences, Magyar tudósok körútja 2, H3660, 23-3650, 96, 1117 Budapest, Hungary. Electronic address: kelemen.adam@ttk.mta.hu.

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

PMID:
29910079
DOI:
10.1016/j.bmcl.2018.06.019
[Indexed for MEDLINE]

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