Piperazinyl CCR1 antagonists—optimization of human liver microsome stability

…, RP Gladue, A Guzman-Martinez, MM Hayward…

文献索引：Brown, Matthew F.; Bahnck, Kevin B.; Blumberg, Laura C.; Brissette, William H.; Burrell, Sara A.; Driscoll, James P.; Fedeles, Flavia; Fisher, Michael B.; Foti, Robert S.; Gladue, Ronald P.; Guzman-Martinez, Aikomari; Hayward, Matthew M.; Lira, Paul D.; Lillie, Brett M.; Lu, Yi; Lundquist, Greg D.; McElroy, Eric B.; McGlynn, Molly A.; Paradis, Timothy J.; Poss, Christopher S.; Roache, James H.; Shavnya, Andrei; Shepard, Richard M.; Trevena, Kristen A.; Tylaska, Laurie A. Bioorganic and Medicinal Chemistry Letters, 2007 , vol. 17, # 11 p. 3109 - 3112

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被引用次数: 15

摘要

... Compound 5a was settled on as the minimum pharmacophore as removal of either the 4-F, 4-Cl or 2-piperazinyl methyl groups led to a substantial loss of potency in binding and/or functional chemotaxis assays. ... In general, compounds described herein with Clog D values ⩽2 provided in vitro human clearance values (Cl b ) at or near the lower limit of the assay utilized. ... References and notes. 1; RP Gladue, SH Zwillich, AT Clucas, MF Brown; Curr. Opin. Investig. ...