Abstract
A series of nicotinamide N-oxides was synthesized and shown to be novel, potent, and selective antagonists of the CXCR2 receptor. Furthermore, these compounds showed significant functional activity against GRO-alpha-driven human neutrophil chemotaxis. Compounds of this class may be useful for the treatment of inflammatory, auto-immune, and allergic disorders.
MeSH terms
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Autoimmune Diseases / drug therapy
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Binding Sites / physiology
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Chemokine CXCL1
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Chemokines, CXC*
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Chemotactic Factors / metabolism*
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Chemotaxis / drug effects*
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Chemotaxis / physiology
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Growth Substances / metabolism*
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Humans
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Hypersensitivity / drug therapy
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Inflammation / drug therapy
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Inhibitory Concentration 50
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Intercellular Signaling Peptides and Proteins*
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Interleukin-8 / metabolism*
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Neutrophils / physiology
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Niacinamide / analogs & derivatives*
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Niacinamide / chemical synthesis
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Niacinamide / pharmacology*
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Protein Binding / physiology
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Receptors, Interleukin-8B / antagonists & inhibitors*
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Structure-Activity Relationship
Substances
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CXCL1 protein, human
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Chemokine CXCL1
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Chemokines, CXC
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Chemotactic Factors
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Growth Substances
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Intercellular Signaling Peptides and Proteins
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Interleukin-8
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Receptors, Interleukin-8B
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Niacinamide
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nicotinamide N-oxide