960312-69-0Relevant articles and documents
Development of CXCR3 antagonists. Part 2: Identification of 2-amino(4-piperidinyl)azoles as potent CXCR3 antagonists
Watson, Robert J.,Allen, Daniel R.,Birch, Helen L.,Chapman, Gayle A.,Hannah, Duncan R.,Knight, Roland L.,Meissner, Johannes W.G.,Owen, David A.,Thomas, Elizabeth J.
, p. 6806 - 6810 (2008/09/16)
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 5.4 h.