1191066-56-4Relevant articles and documents
Discovery of a novel series of CXCR3 antagonists
Crosignani, Stefano,Missotten, Marc,Cleva, Christophe,Dondi, Ruggero,Ratinaud, Yann,Humbert, Yves,Mandal, Ashis Baran,Bombrun, Agns,Power, Christine,Chollet, Andre,Proudfoot, Amanda
scheme or table, p. 3614 - 3617 (2010/09/17)
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.