Design and optimization of imidazole derivatives as potent CXCR3 antagonists
Xiaohui Du1, Xiaoqi Chen, Jeffrey T Mihalic
1Amgen Inc. 1120 Veterans Boulevard, South San Francisco, CA 94080, USA.
Abstract:
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.
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