Development of selective agents targeting serotonin 5HT 1A receptors with subnanomolar activities based on a coumarin core

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...

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Bibliographic Details
Published in:MedChemComm 2017-08, Vol.8 (8), p.1690-1696
Main Authors: Ostrowska, K, Grzeszczuk, D, Głuch-Lutwin, M, Gryboś, A, Siwek, A, Dobrzycki, Ł, Trzaskowski, B
Format: Article
Language:English
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Summary: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-HT receptor (0.3-1.0 nM) and good selectivity against the 5-HT 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.
ISSN:2040-2503
2040-2511
DOI:10.1039/c7md00281e