Pégurier Cécile, Collart Philippe, Danhaive Pierre, Defays Sabine, Gillard Michel, Gilson Frédéric, Kogej Thierry, Pasau Patrick, Van Houtvin Nathalie, Van Thuyne Marc, van Keulen BerendJan
UCB Pharma SA, R&D, Chemin du Foriest, B-1420 Braine-L'Alleud, Belgium.
Bioorg Med Chem Lett. 2007 Aug 1;17(15):4228-31. doi: 10.1016/j.bmcl.2007.05.035. Epub 2007 May 17.
The discovery and optimization of a novel class of potent CCR3 antagonists is described. Details of synthesis and SAR are given together with some ADME properties of selected compounds. An optimal balance between activities, physicochemical properties, and in vitro metabolic stability was reached by the proper choice of substituents.