N-Arylalkylpiperidine urea derivatives as CC chemokine receptor-3 (CCR3) antagonists

Douglas G Batt; Gregory C Houghton; John Roderick; Joseph B Santella 3rd; Dean A Wacker; Patricia K Welch; Yevgeniya I Orlovsky; Eric A Wadman; James M Trzaskos; Paul Davies; Carl P Decicco; Percy H Carter

doi:10.1016/j.bmcl.2004.11.006

N-Arylalkylpiperidine urea derivatives as CC chemokine receptor-3 (CCR3) antagonists

Bioorg Med Chem Lett. 2005 Feb 1;15(3):787-91. doi: 10.1016/j.bmcl.2004.11.006.

Authors

Douglas G Batt¹, Gregory C Houghton, John Roderick, Joseph B Santella 3rd, Dean A Wacker, Patricia K Welch, Yevgeniya I Orlovsky, Eric A Wadman, James M Trzaskos, Paul Davies, Carl P Decicco, Percy H Carter

Affiliation

¹ dBristol-Myers Squibb, Pharmaceutical Research Institute, PO Box 4000, Princeton, NJ 08543-4000, USA. douglas.batt@bms.com

PMID: 15664858
DOI: 10.1016/j.bmcl.2004.11.006

Abstract

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.

MeSH terms

Calcium Signaling / drug effects
Chemokine CCL11
Chemokines, CC / pharmacology
Drug Interactions
Eosinophils / drug effects
Humans
Inhibitory Concentration 50
Piperidines / chemical synthesis*
Piperidines / pharmacology
Protein Binding
Receptors, CCR3
Receptors, Chemokine / antagonists & inhibitors*
Structure-Activity Relationship
Urea / chemical synthesis*
Urea / pharmacology

Substances

CCL11 protein, human
CCR3 protein, human
Chemokine CCL11
Chemokines, CC
Piperidines
Receptors, CCR3
Receptors, Chemokine
Urea