Small molecule antagonists of the CCR2b receptor. Part 2: discovery process and initial structure–activity relationships of diamine derivatives

WJ Moree, K Kataoka, MM Ramirez-Weinhouse…

文献索引：Moree, Wilna J.; Kataoka, Ken-Ichiro; Ramirez-Weinhouse, Michele M.; Shiota, Tatsuki; Imai, Minoru; Sudo, Masaki; Tsutsumi, Takaharu; Endo, Noriaki; Muroga, Yumiko; Hada, Takahiko; Tanaka, Hiroko; Morita, Takuya; Greene, Jonathan; Barnum, Doug; Saunders, John; Kato, Yoshinori; Myers, Peter L.; Tarby, Christine M. Bioorganic and Medicinal Chemistry Letters, 2004 , vol. 14, # 21 p. 5413 - 5416

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被引用次数: 49

摘要

Structure–activity relationships (SAR) of a weakly active class of CCR2b inhibitors were utilized to initiate a lead evolution program employing the Drug Discovery Engine™. Several alternative structural series have been discovered that display nanomolar activity in the CCR2b binding and CCR2b-mediated chemotaxis assays.