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

Jason G Kettle; Alan W Faull; Andy J Barker; D Huw Davies; Michael A Stone

doi:10.1016/j.bmcl.2003.10.049

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

Bioorg Med Chem Lett. 2004 Jan 19;14(2):405-8. doi: 10.1016/j.bmcl.2003.10.049.

Authors

Jason G Kettle¹, Alan W Faull, Andy J Barker, D Huw Davies, Michael A Stone

Affiliation

¹ AstraZeneca, Mereside, Alderley Park, Cheshire SK10 4TG, Macclesfield, UK. [email protected]

PMID: 14698169
DOI: 10.1016/j.bmcl.2003.10.049

Abstract

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.

MeSH terms

Benzyl Compounds / metabolism
Benzyl Compounds / pharmacology*
Carboxylic Acids / metabolism
Carboxylic Acids / pharmacology*
Indoles / metabolism
Indoles / pharmacology*
Protein Binding / physiology
Receptors, CCR2
Receptors, Chemokine / antagonists & inhibitors*
Receptors, Chemokine / metabolism*

Substances

Benzyl Compounds
Carboxylic Acids
Indoles
Receptors, CCR2
Receptors, Chemokine