Imidazolylpyrimidine based CXCR2 chemokine receptor antagonists.
作者信息
Ho Koc-Kan, Auld Douglas S, Bohnstedt Adolph C, Conti Paolo, Dokter Wim, Erickson Shawn, Feng Daming, Inglese Jim, Kingsbury Celia, Kultgen Steven G, Liu Rong-Qiang, Masterson Christopher M, Ohlmeyer Michael, Rong Yajing, Rooseboom Martijn, Roughton Andrew, Samama Philippe, Smit Martin-Jan, Son Ellen, van der Louw Jaap, Vogel Gerard, Webb Maria, Wijkmans Jac, You Ming
机构信息
Pharmacopeia Drug Discovery, Inc., PO Box 5350, Princeton, NJ 08543-5350, USA.
出版信息
Bioorg Med Chem Lett. 2006 May 15;16(10):2724-8. doi: 10.1016/j.bmcl.2006.02.028. Epub 2006 Mar 15.
An imidazolylpyrimidine was identified in a CXCR2 chemokine receptor antagonist screen and was optimized for potency, in vitro metabolic stability, and oral bioavailability. It was found that subtle structural modification within the series affected the oral bioavailability. Potent and orally available CXCR2 antagonists are herein reported.
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