| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 10588821 | Bioorganic & Medicinal Chemistry Letters | 2010 | 4 Pages |
Abstract
The discovery of a novel series of CXCR3 antagonists is described. Starting from an HTS positive, iterative optimization gave potent compounds (IC50 15Â nM in a chemotaxis assay). The strategy employed to improve the metabolic stability of these derivatives is described.
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Stefano Crosignani, Marc Missotten, Christophe Cleva, Ruggero Dondi, Yann Ratinaud, Yves Humbert, Ashis Baran Mandal, Agnès Bombrun, Christine Power, André Chollet, Amanda Proudfoot,