Bioorganic and Medicinal Chemistry Letters p. 6806 - 6810 (2007)
Update date:2022-08-05
Topics: Antagonist Potent Development Identification Experimental Chemical CXCR3 2-amino(4-piperidinyl)azoles Part 2
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.
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.
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