- Design and synthesis of novel CCR3 antagonists.
Design and synthesis of novel CCR3 antagonists.
Bioorganic & medicinal chemistry letters (2003-09-25)
Leyi Gong, J Heather Hogg, James Collier, Robert S Wilhelm, Carol Soderberg
PMID14505678
ABSTRACT
As part of our investigation into the development of potent CCR3 antagonists, a series of piperidine analogues was designed and prepared. Exploration of the piperidine core examined both the basicity and the location of a nitrogen, as well as conformational variants. The bicyclo-piperidine 24c was found to be the most potent inhibitor of CCR3 with an IC(50) of 0.0082 microM in the binding assay and 0.0024 microM in the chemotaxis assay.
MATERIALS