Design and synthesis of novel CCR3 antagonists |
| |
Authors: | Gong Leyi Hogg J Heather Collier James Wilhelm Robert S Soderberg Carol |
| |
Affiliation: | Department of Medicinal Chemistry, Roche Palo Alto, Palo Alto, CA 94304, USA. leyi.gong@roche.com |
| |
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. |
| |
Keywords: | |
本文献已被 ScienceDirect PubMed 等数据库收录! |
|