Design and synthesis of novel CCR3 antagonists

…, JH Hogg, J Collier, RS Wilhelm, C Soderberg

Index: Gong, Leyi; Hogg, J. Heather; Collier, James; Wilhelm, Robert S.; Soderberg, Carol Bioorganic and Medicinal Chemistry Letters, 2003 , vol. 13, # 20 p. 3597 - 3600

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Citation Number: 13

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 IC50 of 0.0082 μM in the binding assay and 0.0024 μM in the chemotaxis assay.