作为强效CXCR3拮抗剂的咪唑衍生物的设计与优化
Design and optimization of imidazole derivatives as potent CXCR3 antagonists.
作者信息
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
机构信息
Amgen Inc. 1120 Veterans Boulevard, South San Francisco, CA 94080, USA.
出版信息
Bioorg Med Chem Lett. 2008 Jan 15;18(2):608-13. doi: 10.1016/j.bmcl.2007.11.072. Epub 2007 Nov 28.
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.
一系列咪唑衍生物已被设计并优化，以实现对CXCR3的拮抗作用、改善药代动力学性质，并减少谷胱甘肽缀合物的形成。我们的研究工作导致发现了具有良好药代动力学性质的强效CXCR3拮抗剂。这些化合物是用于CXCR3功能体内研究的有用工具。
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