Tetrahydroquinoline derivatives as CRTH2 antagonists

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. A series of tetrahydroquinoline-de...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2009-12, Vol.19 (24), p.6840-6844
Hauptverfasser:	Liu, Jiwen, Wang, Yingcai, Sun, Ying, Marshall, Derek, Miao, Shichang, Tonn, George, Anders, Penny, Tocker, Joel, Tang, H. Lucy, Medina, Julio
Format:	Artikel
Sprache:	eng
Schlagworte:	Allergic diseases Antagonists Anti-Allergic Agents - chemistry Anti-Allergic Agents - pharmacokinetics Anti-Allergic Agents - pharmacology Biological and medical sciences Cell Line Cell Shape - drug effects CRTH2 Drug Discovery Eosinophils - drug effects Eosinophils - immunology GPCR Histamine and antagonists. Allergy Humans Lead optimization Medical sciences PGD2 Pharmacology. Drug treatments Quinolines - chemistry Quinolines - pharmacokinetics Quinolines - pharmacology Receptors, Immunologic - antagonists & inhibitors Receptors, Prostaglandin - antagonists & inhibitors SAR Tetrahydroquinoline
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Zusammenfassung:	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. 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.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2009.10.094