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Issue 8, 2017
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Development of selective agents targeting serotonin 5HT1A receptors with subnanomolar activities based on a coumarin core

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Abstract

A series of 18 new 5-[3-(4-aryl-1-piperazinyl)propoxy]coumarin derivatives from the corresponding bromoalkyl derivatives have been designed and synthesized by us using a microwave-assisted protocol. Radioligand binding assays of this series of compounds as well as a previously synthesized series of 17 structurally-similar compounds showed that six systems have very high affinities to the 5-HT1A receptor (0.3–1.0 nM) and good selectivity against the 5-HT2A receptor. Molecular docking, structural studies and structure–activity relationship studies were used to gain more insight into the atomistic details of ligand binding and rationalize the obtained results.

Graphical abstract: Development of selective agents targeting serotonin 5HT1A receptors with subnanomolar activities based on a coumarin core

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Publication details

The article was received on 31 May 2017, accepted on 23 Jun 2017 and first published on 03 Jul 2017


Article type: Research Article
DOI: 10.1039/C7MD00281E
Citation: Med. Chem. Commun., 2017,8, 1690-1696
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    Development of selective agents targeting serotonin 5HT1A receptors with subnanomolar activities based on a coumarin core

    K. Ostrowska, D. Grzeszczuk, M. Głuch-Lutwin, A. Gryboś, A. Siwek, Ł. Dobrzycki and B. Trzaskowski, Med. Chem. Commun., 2017, 8, 1690
    DOI: 10.1039/C7MD00281E

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