Structure–Activity Relationship of Imidazopyridinium Analogues as Antagonists of Neuropeptide S Receptor

…, SJ Dehdashti, A Thorsell, M Heilig, L Bell…

文献索引：Patnaik, Samarjit; Marugan, Juan J.; Liu, Ke; Zheng, Wei; Southall, Noel; Dehdashti, Seameen J.; Thorsell, Annika; Heilig, Markus; Bell, Lauren; Zook, Michelle; Eskay, Bob; Brimacombe, Kyle R.; Austin, Christopher P. Journal of Medicinal Chemistry, 2013 , vol. 56, # 22 p. 9045 - 9056

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被引用次数: 4

摘要

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 ...