2. Academic Validation
  3. Structure-activity relationship of imidazopyridinium analogues as antagonists of neuropeptide s receptor

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

  • J Med Chem. 2013 Nov 27;56(22):9045-56. doi: 10.1021/jm400904m.
Samarjit Patnaik 1,  Juan J Marugan,  Ke Liu,  Wei Zheng,  Noel Southall,  Seameen J Dehdashti,  Annika Thorsell,  Markus Heilig,  Lauren Bell,  Michelle Zook,  Bob Eskay,  Kyle R Brimacombe,  Christopher P Austin
Affiliations

Affiliation

  • 1 National Center for Advancing Translational Sciences, National Institutes of Health , 9800 Medical Center Drive, Rockville, Maryland 20850, United States .
PMID: 24171469 DOI: 10.1021/jm400904m
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.

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