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

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS（2012）

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摘要

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. (C) 2011 Elsevier Ltd. All rights reserved.

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关键词

FPR1 antagonist,Small molecule,Hepatocyte media loss assay

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