Optimization of the heterocyclic core of the quinazolinone-derived CXCR3 antagonists.
作者信息
Li An-Rong, Johnson Michael G, Liu Jiwen, Chen Xiaoqi, Du Xiaohui, Mihalic Jeffrey T, Deignan Jeffrey, Gustin Darin J, Duquette Jason, Fu Zice, Zhu Liusheng, Marcus Andrew P, Bergeron Phillipe, McGee Lawrence R, Danao Jay, Lemon Bryan, Carabeo Teresa, Sullivan Timothy, Ma Ji, Tang Liang, 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):688-93. doi: 10.1016/j.bmcl.2007.11.060. Epub 2007 Nov 21.
A series of six-six and six-five fused heterocyclic CXCR3 antagonists has been synthesized and their activities evaluated in an [(125)I]-IP-10 displacement assay and an ITAC mediated in vitro cell migration assay. The pharmacokinetic properties of several top compounds have also been studied. This effort led to the discovery of compounds with increased potency and improved pharmacokinetic properties that could serve as useful tools to study the role of the CXCR3 receptor in vivo.
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