Abstract
It is well known that both acute and chronic autoimmune inflammatory disorders arise following a breakdown in control of neutrophil activation and recruitment. In the search for new anti-inflammatory agents, we synthesized some new 2-phenyl-2,3-dihydro-1H-imidazo[1,2-b]pyrazole derivatives and tested them in vitro in order to evaluate their ability to interfere with human neutrophil functions. All tested compounds showed strong inhibition of fMLP-OMe-induced chemotaxis, although they appeared unable to block degranulation and the fMLP-OMe-induced respiratory burst, and were inactive in binding experiments.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Anti-Inflammatory Agents / pharmacology
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Binding, Competitive
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Chemistry, Pharmaceutical / methods*
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Chemotaxis / drug effects*
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Dose-Response Relationship, Drug
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Drug Design
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Humans
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Inhibitory Concentration 50
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Kinetics
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Models, Chemical
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N-Formylmethionine Leucyl-Phenylalanine / antagonists & inhibitors*
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N-Formylmethionine Leucyl-Phenylalanine / chemistry*
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Neutrophils / drug effects*
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Neutrophils / metabolism
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Protein Binding
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Pyrazoles / chemistry*
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Signal Transduction
Substances
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Anti-Inflammatory Agents
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Pyrazoles
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N-Formylmethionine Leucyl-Phenylalanine
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2,3-dihydro-1H-imidazo(1,2-b)pyrazole