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J Med Chem. 2013 Nov 27;56(22):9045-56. doi: 10.1021/jm400904m. Epub 2013 Nov 11.

Structure-activity relationship of imidazopyridinium analogues as antagonists of neuropeptide s receptor.

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1
National Center for Advancing Translational Sciences, National Institutes of Health , 9800 Medical Center Drive, Rockville, Maryland 20850, United States .

Abstract

The discovery and characterization of a novel chemical series of phosphorothioyl-containing imidazopyridines as potent neuropeptide S receptor antagonists is presented. The synthesis of analogues and their structure-activity relationship with respect to the Gq, Gs, and ERK pathways is detailed. The pharmacokinetics and in vivo efficacy of a potent analogue in a food intake rodent model are also included, underscoring its potential therapeutic value for the treatment of sleep, anxiety, and addiction disorders.

PMID:
24171469
PMCID:
PMC4877059
DOI:
10.1021/jm400904m
[Indexed for MEDLINE]
Free PMC Article

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