Discovery and evaluation of a novel monocyclic series of CXCR2 antagonists
Rupert P Austin1, Colin Bennion1, Roger V Bonnert1
1AstraZeneca R&D Charnwood, Bakewell Road, Loughborough, Leicestershire, LE11 5RH, UK.
Bioorganic & Medicinal Chemistry Letters
|February 25, 2015
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.
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