N-Benzylindole-2-carboxylic acids: potent functional antagonists of the CCR2b chemokine receptor

Screening of the corporate database led to the discovery of a novel series of N-benzylindole-2-carboxylic acid CCR2b chemokine receptor antagonists. These compounds demonstrate high affinity and functional inhibition of the CCR2b receptor. A discussion of the structure–activity relationships is pres...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2004-01, Vol.14 (2), p.405-408
Hauptverfasser:	Kettle, Jason G., Faull, Alan W., Barker, Andy J., Davies, D.Huw, Stone, Michael A.
Format:	Artikel
Sprache:	eng
Schlagworte:	Antagonist Benzyl Compounds - metabolism Benzyl Compounds - pharmacology Biological and medical sciences Carboxylic Acids - metabolism Carboxylic Acids - pharmacology CCR2b Chemokine Indoles - metabolism Indoles - pharmacology Medical sciences Miscellaneous Pharmacology. Drug treatments Protein Binding - physiology Receptors, CCR2 Receptors, Chemokine - antagonists & inhibitors Receptors, Chemokine - metabolism
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Beschreibung
Zusammenfassung:	Screening of the corporate database led to the discovery of a novel series of N-benzylindole-2-carboxylic acid CCR2b chemokine receptor antagonists. These compounds demonstrate high affinity and functional inhibition of the CCR2b receptor. A discussion of the structure–activity relationships is presented, together with evidence for a highly selective receptor binding profile. Graphic
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2003.10.049