Design and synthesis of novel CCR3 antagonists.
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.
D015195:Drug Design; D010880:Piperidines / Q000138:chemical synthesis / Q000737:chemistry*; D054397:Receptors, CCR3; D019707:Receptors, Chemokine / Q000037:antagonists & inhibitors*
D010880:Piperidines; D054397:Receptors, CCR3; D019707:Receptors, Chemokine