Bioorganic and Medicinal Chemistry Letters p. 3597 - 3600 (2003)
Update date:2022-07-29
Topics:
Gong, Leyi
Hogg, J. Heather
Collier, James
Wilhelm, Robert S.
Soderberg, Carol
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.
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