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 presented, together with evidence for a highly selective receptor binding profile.
Kettle
Jason G
JG
AstraZeneca, Mereside, Alderley Park, Cheshire SK10 4TG, Macclesfield, UK. jason.kettle@astrazeneca.com
Faull
Alan W
AW
Barker
Andy J
AJ
Davies
D Huw
DH
Stone
Michael A
MA
D001593:Benzyl Compounds / Q000378:metabolism / Q000494:pharmacology*; D002264:Carboxylic Acids / Q000378:metabolism / Q000494:pharmacology*; D007211:Indoles / Q000378:metabolism / Q000494:pharmacology*; D011485:Protein Binding / Q000502:physiology; D054390:Receptors, CCR2; D019707:Receptors, Chemokine / Q000037:antagonists & inhibitors* / Q000378:metabolism*
D001593:Benzyl Compounds; D002264:Carboxylic Acids; D007211:Indoles; D054390:Receptors, CCR2; D019707:Receptors, Chemokine