Abstract
A series of 3-substituted N,N'-diarylureas was prepared and the structure-activity relationship relative to CXCR2 receptor affinity as well as their pharmacokinetic properties were examined. In vitro microsomal metabolism studies indicated that the lower clearance rates of the 3-sulfonamido-substituted compounds were most likely due to the suppression of glucuronidation.
MeSH terms
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Administration, Oral
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Animals
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Biological Availability
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Humans
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Microsomes, Liver / drug effects
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Microsomes, Liver / metabolism
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Protein Binding / drug effects
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Protein Binding / physiology
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Rats
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Rats, Sprague-Dawley
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Receptors, Interleukin-8B / antagonists & inhibitors*
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Receptors, Interleukin-8B / metabolism
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Sulfonylurea Compounds / chemistry*
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Sulfonylurea Compounds / metabolism
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Sulfonylurea Compounds / pharmacology
Substances
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Receptors, Interleukin-8B
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Sulfonylurea Compounds