Bioorganic & Medicinal Chemistry Letters 2003-10-20

Design and synthesis of novel CCR3 antagonists.

Leyi Gong, J Heather Hogg, James Collier, Robert S Wilhelm, Carol Soderberg

文献索引：Bioorg. Med. Chem. Lett. 13(20) , 3597-600, (2003)

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摘要

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.