Publication | Open Access
Evaluation of Potent and Selective Small-Molecule Antagonists for the CXCR2 Chemokine Receptor
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Citations
14
References
2004
Year
ImmunologyPharmacotherapyDrug ResistanceInflammationCxcr2 Chemokine ReceptorEar EdemaSelective Cxcr2 AntagonistAllergyGranulocyteReceptor (Biochemistry)Mechanism Of ActionPharmacological AgentNon-peptide LigandPharmacologyCxcr2 ReceptorAnti-inflammatoryFunctional SelectivitySelective Small-molecule AntagonistsMedicineDrug Discovery
N,N'-Diarylureas were prepared, and the structure-activity relationship relative to the CXCR2 receptor was examined. This led to the identification of a potent and highly selective CXCR2 antagonist, which in addition was shown to be functionally active both in vitro against human neutrophils and in vivo in rabbit models of ear edema and neutropenia.
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