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Bioorg Med Chem Lett. 2014 Feb 1;24(3):828-30. doi: 10.1016/j.bmcl.2013.12.087. Epub 2013 Dec 28.

Structure-activity relationships of N-substituted 4-(trifluoromethoxy)benzamidines with affinity for GluN2B-containing NMDA receptors.

Author information

1
School of Chemistry, The University of Sydney, NSW 2006, Australia.
2
School of Chemistry, The University of Sydney, NSW 2006, Australia; Brain and Mind Research Institute, Sydney, NSW 2050, Australia.
3
CSIRO Materials Science & Engineering, Ian Wark Laboratory, Bayview Avenue, Clayton, Victoria 3168, Australia.
4
Department of Radiology & Nuclear Medicine, VU University Medical Centre, Amsterdam 1081HV, The Netherlands.
5
School of Chemistry, The University of Sydney, NSW 2006, Australia; Brain and Mind Research Institute, Sydney, NSW 2050, Australia; Discipline of Medical Radiation Sciences, University of Sydney, NSW 2006, Australia. Electronic address: michael.kassiou@sydney.edu.au.

Abstract

GluN2B subtype-selective NMDA antagonists represent promising therapeutic targets for the symptomatic treatment of multiple CNS pathologies. A series of N-benzyl substituted benzamidines were synthesised and the benzyl ring was further replaced with various polycyclic moieties. Compounds were evaluated for activity at GluN2B containing NMDA receptors where analogues 9, 12, 16 and 18 were the most potent of the series, replacement of the benzyl ring with polycycles resulted in a complete loss of activity.

KEYWORDS:

Amidine; CNS; GluN2B; NMDA; Structure–activity relationships

PMID:
24412068
DOI:
10.1016/j.bmcl.2013.12.087
[Indexed for MEDLINE]

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