Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 19, Issue 24, Pages 6840-6844Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2009.10.094
Keywords
CRTH2; PGD2; Antagonists; GPCR; Allergic diseases; Tetrahydroquinoline; SAR; Lead optimization
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A series of tetrahydroquinoline-derived inhibitors of the CRTH2 receptor was discovered by a high throughput screen. Optimization of these compounds for potency and pharmacokinetic properties led to the discovery of potent and orally bioavailable CRTH2 antagonists. (C) 2009 Elsevier Ltd. All rights reserved.
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