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Design and optimization of imidazole derivatives as potent CXCR3 antagonists |
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| Authors: | Du Xiaohui Chen Xiaoqi Mihalic Jeffrey T Deignan Jeffrey Duquette Jason Li An-Rong Lemon Bryan Ma Ji Miao Shichang Ebsworth Karen Sullivan Timothy J Tonn George Collins Tassie L Medina Julio C |
| Affiliation: | Amgen 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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