Title of article
Development of CXCR3 antagonists. Part 2: Identification of 2-amino(4-piperidinyl)azoles as potent CXCR3 antagonists
Author/Authors
Robert J. Watson، نويسنده , , Daniel R. Allen، نويسنده , , Helen L. Birch، نويسنده , , Gayle A. Chapman، نويسنده , , Duncan R. Hannah، نويسنده , , Roland L. Knight، نويسنده , , Johannes W.G. Meissner، نويسنده , , David A. Owen، نويسنده , , Elizabeth J. Thomas، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2007
Pages
5
From page
6806
To page
6810
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 5.4 h.
Keywords
CXCR3 antagonist , Benzazole , optimisation , Pharmacokinetics , (Piperidinyl)azoles
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2007
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
798890
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