Lead optimisation of pyrazoles as novel FPR1 antagonists. | LitMetric

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Lead optimisation of pyrazoles as novel FPR1 antagonists. | LitMetric

Lead optimisation of pyrazoles as novel FPR1 antagonists.

Andrew D Morley Sarah King Bryan Roberts Sarah Lever Barry Teobald Adrian Fisher Tony Cook Beth Parker Mark Wenlock Caroline Phillips Ken Grime

Bioorg Med Chem Lett

Chemistry Department, AstraZeneca R&D Charnwood, Bakewell Road, Loughborough LE11 5RH, UK.

Published: January 2012

Optimisation of a series of pyrazole inhibitors of the human FPR1 receptor has been achieved. The use of an in vitro media loss assay was utilised to identify sub-series with more robust DMPK profiles. These were subsequently improved to generate analogues with attractive overall profiles.

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http://dx.doi.org/10.1016/j.bmcl.2011.10.090	DOI Listing

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