Abstract
Structure-activity studies on lead cyclobutenedione 3 led to the discovery of 4 (SCH 527123), a potent, orally bioavailable CXCR2/CXCR1 receptor antagonist with excellent cell-based activity. Compound 4 displayed good oral bioavailability in rat and may be a potential therapeutic agent for the treatment of various inflammatory diseases.
MeSH terms
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Administration, Oral
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Animals
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Benzamides / administration & dosage
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Benzamides / chemical synthesis
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Benzamides / pharmacology*
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Biological Availability
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Cyclobutanes / administration & dosage
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Cyclobutanes / chemical synthesis
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Cyclobutanes / pharmacology*
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Molecular Structure
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Rats
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Receptors, Interleukin-8A / antagonists & inhibitors*
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Receptors, Interleukin-8A / metabolism
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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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2-hydroxy-N,N-dimethyl-3-(2-((1-(5-methylfuran-2-yl)propyl)amino)-3,4-dioxocyclobut-1-enylamino)benzamide
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Benzamides
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Cyclobutanes
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Receptors, Interleukin-8A
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Receptors, Interleukin-8B
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benzamide