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Synthesis and receptor binding studies of some new arylcarboxamide derivatives as sigma-1 ligands

ZAMPIERI, DANIELE
•
LAURINI, ERIK
•
VIO, LUCIANO
altro
MAMOLO, MARIA GRAZIA
2014
  • journal article

Periodico
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Abstract
We describe here the synthesis and the binding interaction with simga1 and sigma2 receptors of a series of new arylcarboxamide derivatives variously substituted on the aromatic portions. Maintaining a partial scaffold of a series of compounds previously synthesized by us, we evaluate the effect of the substitution on sigma binding. The synthesized compounds have been tested to estimate their affinity and selectivity toward sigma1 and sigma2 receptors. Two out of 16 derivatives showed an interesting sigma1 affinity (21.2 and 13.6 nM - compounds 2m and 2p) and a good selectivity (Ki(sigma2) / Ki(sigma1) >140 and >40 respectively).
DOI
10.1016/j.bmcl.2014.01.032
WOS
WOS:000331196600001
Archivio
http://hdl.handle.net/11368/2760961
info:eu-repo/semantics/altIdentifier/scopus/2-s2.0-84893779615
Diritti
closed access
license:digital rights management non definito
FVG url
https://arts.units.it/request-item?handle=11368/2760961
Soggetti
  • sigma receptor

  • sigma1 model

  • computer assisted dru...

  • homology modeling

Web of Science© citazioni
9
Data di acquisizione
Mar 25, 2024
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