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Discovery of potent and orally bioavailable N,N'-diarylurea antagonists for the CXCR2 chemokine receptor.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2004 Sep 06; Vol. 14 (17), pp. 4375-8. - Publication Year :
- 2004
-
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.
- Subjects :
- Administration, Oral
Animals
Biological Availability
Humans
Microsomes, Liver drug effects
Microsomes, Liver metabolism
Protein Binding drug effects
Protein Binding physiology
Rats
Rats, Sprague-Dawley
Receptors, Interleukin-8B metabolism
Sulfonylurea Compounds metabolism
Sulfonylurea Compounds pharmacology
Receptors, Interleukin-8B antagonists & inhibitors
Sulfonylurea Compounds chemistry
Subjects
Details
- Language :
- English
- ISSN :
- 0960-894X
- Volume :
- 14
- Issue :
- 17
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 15357956
- Full Text :
- https://doi.org/10.1016/j.bmcl.2004.06.097