Comparison of N,N'-diarylsquaramides and N,N'-diarylureas as antagonists of the CXCR2 chemokine receptor

Autor:	James J. Foley, Brent W. Mccleland, Miriam Burman, Roderick S. Davis, Gary J. Stelman, Martin Rogers, Palovich Michael R, Michelle L. Werner, Keith W. Ward, Jakob Busch-Petersen, Kevin L. Salyers, Theresa J. Roethke, Dulcie B. Schmidt, Leonard M. Azzarano, Henry M. Sarau, Widdowson Katherine L, Peter D. Gorycki
Rok vydání:	2006
Předmět:	Chemical Phenomena Stereochemistry medicine.drug_class Clinical Biochemistry Substituent Pharmaceutical Science Carboxamide CHO Cells Biochemistry Chemical synthesis Mass Spectrometry Receptors Interleukin-8B Rats Sprague-Dawley chemistry.chemical_compound Chemokine receptor Structure-Activity Relationship Cricetulus Phenols Cricetinae Drug Discovery medicine Structure–activity relationship Animals Urea CXC chemokine receptors Molecular Biology chemistry.chemical_classification Sulfonamides Chemistry Physical Organic Chemistry Antagonist Sulfonamide Rats chemistry Molecular Medicine Indicators and Reagents Cyclobutanes
Zdroj:	Bioorganicmedicinal chemistry letters. 17(6)
ISSN:	0960-894X
Popis:	N,N'-diarylsquaramides were prepared and evaluated as antagonists of CXCR2. The compounds were found to be potent and selective antagonists of CXCR2. Significant differences in SAR was observed relative to the previously described N,N'-diarylurea series. As was the case in the N,N'-diarylurea series, placing sulfonamide substituent adjacent to the acidic phenol significantly reduced the clearance in rat pharmacokinetic studies.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9dd7a2d57ef623074395364e347a7faf https://pubmed.ncbi.nlm.nih.gov/17236763 Zobrazit plný text záznamu Full Text from ScienceDirect