Abstract
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.
Copyright © 2011 Elsevier Ltd. All rights reserved.
MeSH terms
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Animals
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Chemistry, Pharmaceutical / methods
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Chemistry, Physical / methods
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Drug Design
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Hepatocytes / cytology
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Humans
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Inhibitory Concentration 50
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Male
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Microsomes, Liver / metabolism
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Models, Chemical
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Pyrazoles / chemical synthesis*
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Pyrazoles / pharmacology*
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Rats
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Rats, Sprague-Dawley
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Receptors, Formyl Peptide / antagonists & inhibitors*
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Receptors, Formyl Peptide / chemistry
Substances
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FPR1 protein, human
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Pyrazoles
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Receptors, Formyl Peptide