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.
MeSH terms
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Animals
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Chromatography, High Pressure Liquid
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Drug Design
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Humans
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Imidazoles / chemistry*
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Imidazoles / pharmacokinetics
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Imidazoles / pharmacology*
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Mice
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Mice, Knockout
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Rats
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Receptors, CXCR3 / antagonists & inhibitors*
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Receptors, CXCR3 / genetics
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Receptors, CXCR3 / physiology
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Structure-Activity Relationship
Substances
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Cxcr3 protein, mouse
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Imidazoles
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Receptors, CXCR3