Issue 12, 2011
From the journal:

MedChemComm

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

María Barceló,a   Enrique Raviña,a   María J. Varela,b   José Brea,b   María I. Lozab  and  Christian F. Masaguer*a  

* Corresponding authors

a Departamento de Química Orgánica, Laboratorio de Química Farmacéutica, Facultad de Farmacia, Universidad de Santiago de Compostela, Santiago de Compostela, Spain
E-mail: christianf.masaguer@usc.es
Fax: +34-881-594628
Tel: +34-881-815099

b Departamento de Farmacología, Facultad de Farmacia, Universidad de Santiago de Compostela, Santiago de Compostela, Spain

Abstract

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.

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

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Article information

DOI
https://doi.org/10.1039/C1MD00202C
Article type
Concise Article
Submitted
06 Aug 2011
Accepted
12 Sep 2011
First published
11 Oct 2011

Med. Chem. Commun., 2011,2, 1194-1200

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

M. Barceló, E. Raviña, M. J. Varela, J. Brea, M. I. Loza and C. F. Masaguer, Med. Chem. Commun., 2011, 2, 1194 DOI: 10.1039/C1MD00202C

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