N-Arylalkylpiperidine urea derivatives as CC chemokine receptor-3 (CCR3) antagonists.
The synthesis and structure-activity relationships of N-arylalkylpiperidylmethyl ureas as antagonists of the CC chemokine receptor-3 (CCR3) are presented. These compounds displayed potent binding to the receptor as well as functional antagonism of eotaxin-elicited effects on eosinophils.
Batt
Douglas G
DG
dBristol-Myers Squibb, Pharmaceutical Research Institute, PO Box 4000, Princeton, NJ 08543-4000, USA. douglas.batt@bms.com
Houghton
Gregory C
GC
Roderick
John
J
Santella
Joseph B
JB
Wacker
Dean A
DA
Welch
Patricia K
PK
Orlovsky
Yevgeniya I
YI
Wadman
Eric A
EA
Trzaskos
James M
JM
Davies
Paul
P
Decicco
Carl P
CP
Carter
Percy H
PH
D020013:Calcium Signaling / Q000187:drug effects; D054413:Chemokine CCL11; D019742:Chemokines, CC / Q000494:pharmacology; D004347:Drug Interactions; D004804:Eosinophils / Q000187:drug effects; D006801:Humans; D020128:Inhibitory Concentration 50; D010880:Piperidines / Q000138:chemical synthesis* / Q000494:pharmacology; D011485:Protein Binding; D054397:Receptors, CCR3; D019707:Receptors, Chemokine / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship; D014508:Urea / Q000138:chemical synthesis* / Q000494:pharmacology
C515456:CCL11 protein, human; C515350:CCR3 protein, human; D054413:Chemokine CCL11; D019742:Chemokines, CC; D010880:Piperidines; D054397:Receptors, CCR3; D019707:Receptors, Chemokine; D014508:Urea