4.5 Article

Design and optimization of imidazole derivatives as potent CXCR3 antagonists

Journal

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 18, Issue 2, Pages 608-613

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2007.11.072

Keywords

CXCR3; IP10; ITAC; mig; CXCL9; CXCL10; CXCL1; imidazole; chemokine

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A series of imidazole derivatives have been designed and optimized for CXCR3 antagonism, pharmacokinetic properties, and reduced formation of glutathione conjugates. Our efforts led to the discovery of potent CXCR3 antagonists with good pharmacokinetic properties. These compounds are useful tools for in vivo studies of CXCR3 function. (c) 2007 Elsevier Ltd. All rights reserved.

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