Potent and selective CC-chemokine receptor-2 (CCR2) antagonists as a potential treatment for asthma.
A number of compounds bearing a quaternary ammonium moiety were found to be antagonists with nanomolar binding affinity for the chemokine receptor-2. The structure-activity relationships in the series are described herein along with some detailed characterization of the interesting compounds.
Lagu
Bharat
B
Johnson & Johnson Pharmaceutical Research and Development, Cranbury, NJ 08512, USA. bharat.lagu@novartis.com
Gerchak
Chrissy
C
Pan
Meng
M
Hou
Cuifen
C
Singer
Monica
M
Malaviya
Ravi
R
Matheis
Michele
M
Olini
Gil
G
Cavender
Druie
D
Wachter
Michael
M
D018927:Anti-Asthmatic Agents / Q000627:therapeutic use*; D001249:Asthma / Q000188:drug therapy*; D006801:Humans; D054390:Receptors, CCR2; D019707:Receptors, Chemokine / Q000037:antagonists & inhibitors*
D018927:Anti-Asthmatic Agents; C515334:CCR2 protein, human; D054390:Receptors, CCR2; D019707:Receptors, Chemokine