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ID: ALA1140582

Journal: Bioorg Med Chem Lett

Title: Development of CXCR3 antagonists. Part 2: Identification of 2-amino(4-piperidinyl)azoles as potent CXCR3 antagonists.

Authors: Watson RJ, Allen DR, Birch HL, Chapman GA, Hannah DR, Knight RL, Meissner JW, Owen DA, Thomas EJ.

Abstract: Development of a lead series of piperidinylurea CXCR3 antagonists has led to the identification of molecules with alternative linkages which retain good potency. A novel 5-(piperidin-4-yl)amino-1,2,4-thiadiazole derivative was found to have satisfactory in vitro metabolic stability and to be orally bioavailable in mice, giving high plasma concentrations and a half life of 5.4h.

CiteXplore: 17964154

DOI: 10.1016/j.bmcl.2007.10.029