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. 2015 Apr 1;25(7):1616-20.
doi: 10.1016/j.bmcl.2015.01.067. Epub 2015 Feb 3.

Discovery and evaluation of a novel monocyclic series of CXCR2 antagonists

Rupert P Austin  1 , Colin Bennion  1 , Roger V Bonnert  1 , Lal Cheema  1 , Anthony R Cook  1 , Rhona J Cox  2 , Mark R Ebden  1 , Alasdair Gaw  1 , Ken Grime  3 , Premji Meghani  1 , David Nicholls  4 , Caroline Phillips  4 , Neal Smith  1 , John Steele  3 , Jeffrey P Stonehouse  1
Affiliations

Discovery and evaluation of a novel monocyclic series of CXCR2 antagonists

Rupert P Austin et al. Bioorg Med Chem Lett. .

Abstract

Antagonism of the chemokine receptor CXCR2 has been proposed as a strategy for the treatment of inflammatory diseases such as arthritis, chronic obstructive pulmonary disease and asthma. Earlier series of bicyclic CXCR2 antagonists discovered at AstraZeneca were shown to have low solubility and poor oral bioavailability. In this Letter we describe the design, synthesis and characterisation of a new series of monocyclic CXCR2 antagonists with improved solubility and good pharmacokinetic profiles.

Keywords: CXCR2; Chemokine antagonism; Inflammatory disease; Solubility.

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