Functionalization at position 3 of the phenyl ring of the potent mGluR5 noncompetitive antagonists MPEP

doi:10.1016/j.bmcl.2004.12.047

Bioorganic & Medicinal Chemistry Letters

Volume 15, Issue 4, 15 February 2005, Pages 945-949

https://doi.org/10.1016/j.bmcl.2004.12.047 Get rights and content

Abstract

We described the synthesis and biological evaluation of MPEP analogs functionalized at the position 3 of the phenyl ring. The results point out the limitation in the choice of a functional group at this position; the only substituents leading to retention of activity are NO₂ (IC₅₀ = 13 nM) and CN (IC₅₀ = 8 nM).

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Acknowledgments

This work was supported by the National Institutes of Health (DA16180-01), from Department of Veterans Affairs, National Center for PTSD Alcohol Research Center and NARSAD to GDT and by the National Institute of Mental Health through the Psychoactive Drug Screening Program (N01MH80005) and KO2MH01366 to BLR.

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Functionalization at position 3 of the phenyl ring of the potent mGluR5 noncompetitive antagonists MPEP

Abstract

Graphical abstract

Section snippets

Acknowledgments

Neuropsychopharmacology

Bioorg. Med. Chem. Lett.

Neuropharmacology

Il Farmaco

Bioorg. Med. Chem. Lett.