Tricyclic imidazole antagonists of the Neuropeptide S Receptor

…, K Menzel, M Henault, R Stocco, JJ Renger…

文献索引：Trotter, B. Wesley; Nanda, Kausik K.; Manley, Peter J.; Uebele, Victor N.; Condra, Cindra L.; Gotter, Anthony L.; Menzel, Karsten; Henault, Martin; Stocco, Rino; Renger, John J.; Hartman, George D.; Bilodeau, Mark T. Bioorganic and Medicinal Chemistry Letters, 2010 , vol. 20, # 15 p. 4704 - 4708

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被引用次数: 16

摘要

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, ...