Potential atypical antipsychotics: synthesis, binding affinity and SAR of new heterocyclic bioisosteric butyrophenone analogues as multitarget ligands

A series of 15 heterocyclic butyrophenone analogues was synthesized as potential multi-target ligands. The compounds were assayed for their in vitro human D2 and 5-HT2A receptor affinity, and those compounds exhibiting the highest affinities were evaluated for binding affinity on D1, D3, 5-HT1A, 5-H...

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Bibliographic Details
Published in:MedChemComm 2011-12, Vol.2 (12), p.1194-1200
Main Authors: Barceló, María, Raviña, Enrique, Varela, María J., Brea, José, Loza, María I., Masaguer, Christian F.
Format: Article
Language:English
Subjects:
Neuroleptics
Serotonin S1 receptors
Serotonin S2 receptors
Serotonin S6 receptors
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Summary:A series of 15 heterocyclic butyrophenone analogues was synthesized as potential multi-target ligands. The compounds were assayed for their in vitro human D2 and 5-HT2A receptor affinity, and those compounds exhibiting the highest affinities were evaluated for binding affinity on D1, D3, 5-HT1A, 5-HT2C and 5-HT6 receptors.
ISSN:2040-2503
2040-2511
DOI:10.1039/c1md00202c