Racemic and chiral lactams as potent, selective and functionally active CCR4 antagonists

…, JJ Gaudino, E Laird, D Chantry, C Eberhardt…

文献索引：Newhouse, Bradley; Allen, Shelley; Fauber, Benjamin; Anderson, Aaron S.; Eary, C. Todd; Hansen, Joshua D.; Schiro, Justin; Gaudino, John J.; Laird, Ellen; Chantry, David; Eberhardt, Christine; Burgess, Laurence E. Bioorganic and Medicinal Chemistry Letters, 2004 , vol. 14, # 22 p. 5537 - 5542

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被引用次数: 29

摘要

A series of racemic and chiral, nonracemic lactams that display high binding affinities, functional chemotaxis antagonism, and selectivity toward CCR4 are described. Compound 41, which provides reasonably high blood levels in mice when dosed intraperitoneally, was identified as a useful pharmacological tool to explore the role of CCR4 antagonism in animal models of allergic disease.