Discovery of 3-aryl-5-acylpiperazinyl-pyrazoles as antagonists to the NK 3 receptor

…, S Blanc, S Noël, JM Salvino, MA Ator, G Fraser

文献索引：Hoveyda, Hamid R.; Roy, Marie-Odile; Blanc, Sebastien; Noel, Sophie; Salvino, Joseph M.; Ator, Mark A.; Fraser, Graeme Bioorganic and Medicinal Chemistry Letters, 2011 , vol. 21, # 7 p. 1991 - 1996

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被引用次数: 8

摘要

A series of 3-aryl-5-acylpiperazinyl-pyrazoles (eg, 3a–b) initially identified through a high- throughput screening campaign using the aequorin Ca2+ bioluminescence assay as novel, potent small molecule antagonists of the G protein-coupled human tachykinin NK3 receptor (hNK3-R) is described. Preliminary profiling revealed poor plasma and metabolic stability for these structures in rodents. Further optimization efforts resulted in analogs with improved ...