Discovery of a novel series of CXCR3 antagonists
Stefano Crosignani1, Marc Missotten, Christophe Cleva
1Merck Serono SA, Geneva, Switzerland. stefano.crosignani@merckserono.net
Bioorganic & Medicinal Chemistry Letters
|May 21, 2010
Abstract:
The discovery of a novel series of CXCR3 antagonists is described. Starting from an HTS positive, iterative optimization gave potent compounds (IC(50) 15 nM in a chemotaxis assay). The strategy employed to improve the metabolic stability of these derivatives is described.
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