对CXCR2趋化因子受体强效和选择性小分子拮抗剂的评估。
Evaluation of potent and selective small-molecule antagonists for the CXCR2 chemokine receptor.
作者信息
Widdowson Katherine L, Elliott John D, Veber Daniel F, Nie Hong, Rutledge Melvin C, McCleland Brent W, Xiang Jia-Ning, Jurewicz Anthony J, Hertzberg Robert P, Foley James J, Griswold Don E, Martin Lenox, Lee Judithann M, White John R, Sarau Henry M
机构信息
GlaxoSmithKline, 709 Swedeland Road, King of Prussia, Pennsylvania 19406, USA.
出版信息
J Med Chem. 2004 Mar 11;47(6):1319-21. doi: 10.1021/jm034248l.
N,N'-Diarylureas were prepared, and the structure-activity relationship relative to the CXCR2 receptor was examined. This led to the identification of a potent and highly selective CXCR2 antagonist, which in addition was shown to be functionally active both in vitro against human neutrophils and in vivo in rabbit models of ear edema and neutropenia.
制备了N,N'-二芳基脲，并研究了其与CXCR2受体的构效关系。由此鉴定出一种强效且高度选择性的CXCR2拮抗剂，此外，该拮抗剂在体外对人中性粒细胞以及在兔耳水肿和中性粒细胞减少症模型体内均表现出功能活性。
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