Development of selective agents targeting serotonin 5HT1A receptors with subnanomolar activities based on a coumarin core.
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ABSTRACT:
SUBMITTER: Ostrowska K
PROVIDER: S-EPMC6072470 | biostudies-literature | 2017 Aug
REPOSITORIES: biostudies-literature
Publications
Development of selective agents targeting serotonin 5HT<sub>1A</sub> receptors with subnanomolar activities based on a coumarin core.
Ostrowska K K Grzeszczuk D D Głuch-Lutwin M M Gryboś A A Siwek A A Dobrzycki Ł Ł Trzaskowski B B
MedChemComm 20170703 8
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<sub>1A</sub> receptor (0.3-1.0 nM) and good selectivity against the 5-HT<sub>2A</sub> receptor. Molecula ...[more]
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