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.
journal_name
Medchemcommjournal_title
MedChemCommauthors
Ostrowska K,Grzeszczuk D,Głuch-Lutwin M,Gryboś A,Siwek A,Dobrzycki Ł,Trzaskowski Bdoi
10.1039/c7md00281esubject
Has Abstractpub_date
2017-07-03 00:00:00pages
1690-1696issue
8eissn
2040-2503issn
2040-2511pii
c7md00281ejournal_volume
8pub_type
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