Journal
CURRENT TOPICS IN MEDICINAL CHEMISTRY
Volume 6, Issue 13, Pages 1345-1352Publisher
BENTHAM SCIENCE PUBL LTD
DOI: 10.2174/15680266106061345
Keywords
CXCR2; CXCR1; IL-8; GRO alpha; neutrophil (PMN); chemotaxis; small molecule antagonist
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In the past eight years, numerous series of small molecule CXCR2 and CXCR1 antagonists have been disclosed. These compounds have proved to be effective inhibitors of ELR+ chemokine-induced chemotaxis of neutrophils and other immune cells in vitro and have also been efficacious in several animal models of inflammatory disease. Although some of these compounds have been reported to be in clinical development, no data on clinical studies in patients with inflammatory disease has been revealed to date. This review details the medicinal chemistry and pharmacology of the aforementioned antagonist series.
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