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Tricyclic imidazole antagonists of the Neuropeptide S Receptor

Author:
B. Wesley Trotter   Kausik K. Nanda   Peter J. Manley   Victor N. Uebele   Cindra L. Condra   Anthony L. Gotter   Karsten Menzel   Martin Henault   Rino Stocco   John J. Renger   George D. Hartman   Mark T. Bilodeau  


Journal:
Bioorganic and Medicinal Chemistry Letters


Issue Date:
2010


Abstract(summary):

A new structural class of potent antagonists of the Neuropeptide S Receptor (NPSR) is reported. High-throughput screening identified a tricyclic imidazole antagonist of NPSR, and medicinal chemistry optimization of this structure was undertaken to improve potency against the receptor as well as CNS penetration. Detailed herein are synthetic and medicinal chemistry studies that led to the identification of antagonists 15 and NPSR-PI1, which demonstrate potent in vitro NPSR antagonism and central exposure in vivo.


Page:
4704-4708


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