期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 18, 期 6, 页码 1926-1930出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2008.01.127
关键词
carboxylic acid bioisosteres; acylsulfonamides; acylsulfamides; sulfonylureas; CXCR2; chemokine; IL-8; CXCR1; indole; neutrophils; COPD; asthma
A series of novel acylsulfonamide, acylsulfamide, and sulfonylurea bioisosteres of carboxylic acids were prepared as CXCR2 antagonists. Structure-activity relationships are reported for these series. One potent orally bioavailable inhibitor had excellent PK properties and was active in a lung injury model in hyperoxia-exposed newborn rats. (C) 2008 Elsevier Ltd. All rights reserved.
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