Abstract
We describe herein a novel series of 3-amino-4-hydrazine-cyclobut-3-ene-1,2-diones as potent and selective inhibitors against the CXCR2 chemokine receptor and IL-8-mediated chemotaxis of a CXCR2-expressing cell line. Furthermore, these alkyl-hydrazine series inhibitors such as 5b demonstrated acceptable metabolic stability when incubated in human and rat microsomes.
MeSH terms
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Animals
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Anti-Inflammatory Agents / chemical synthesis*
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Anti-Inflammatory Agents / chemistry
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Anti-Inflammatory Agents / pharmacology
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CHO Cells
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Chemotaxis / drug effects
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Cricetinae
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Cricetulus
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Drug Design
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Humans
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Hydrazines / chemical synthesis*
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Hydrazines / chemistry
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Hydrazines / pharmacology
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Interleukin-8 / metabolism
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Microsomes, Liver / metabolism
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Rats
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Receptors, Interleukin-8B / antagonists & inhibitors*
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Receptors, Interleukin-8B / metabolism
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Structure-Activity Relationship
Substances
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Anti-Inflammatory Agents
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Hydrazines
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Interleukin-8
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Receptors, Interleukin-8B