Imidazolylpyrimidine based CXCR2 chemokine receptor antagonists

…, S Erickson, D Feng, J Inglese, C Kingsbury…

Index: 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 Bioorganic and Medicinal Chemistry Letters, 2006 , vol. 16, # 10 p. 2724 - 2728

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Citation Number: 28

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.