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Bioorg Med Chem Lett. 2008 Jun 1;18(11):3376-81. doi: 10.1016/j.bmcl.2008.04.022. Epub 2008 Apr 13.

Aminopyrazine CB1 receptor inverse agonists.

Author information

1
Neurogen Corporation, 35 Northeast Industrial Road, Branford CT 06405, USA. dwustrow@nrgn.com

Abstract

A series of 5,6-diaryl-2-amino-pyrazines were prepared and found to have antagonist-like properties at the CB1 receptor. Subsequent SAR studies optimized both receptor potency and drug-like properties including solubility and Cytochrome-P450 inhibition potential. Optimized compounds were demonstrated to be inverse agonists and compared in vivo with rimonabant for their ability to inhibit food intake, to occupy central CB1 receptors and to influence hormonal markers associated with obesity.

PMID:
18448340
DOI:
10.1016/j.bmcl.2008.04.022
[Indexed for MEDLINE]

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