| Literature DB >> 25708618 |
Rupert P Austin1, Colin Bennion1, Roger V Bonnert1, Lal Cheema1, Anthony R Cook1, Rhona J Cox2, Mark R Ebden1, Alasdair Gaw1, Ken Grime3, Premji Meghani1, David Nicholls4, Caroline Phillips4, Neal Smith1, John Steele3, Jeffrey P Stonehouse1.
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.Entities:
Keywords: CXCR2; Chemokine antagonism; Inflammatory disease; Solubility
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Year: 2015 PMID： 25708618 DOI： 10.1016/j.bmcl.2015.01.067
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823