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Imidazolylpyrimidine based CXCR2 chemokine receptor antagonists |
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| Authors: | 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 |
| Institution: | Pharmacopeia Drug Discovery, Inc., PO Box 5350, Princeton, NJ 08543-5350, USA. kanho@pcop.com |
| Abstract: | 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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