| Literature DB >> 19632842 |
Jiwen Liu1, Zice Fu, An-Rong Li, Michael Johnson, Liusheng Zhu, Andrew Marcus, Jay Danao, Tim Sullivan, George Tonn, Tassie Collins, Julio Medina.
Abstract
The evaluation of the CXCR3 antagonist AMG 487 in clinic trials was complicated due to the formation of an active metabolite. In this Letter, we will discuss the further optimization of the quinazolinone series that led to the discovery of compounds devoid of the formation of the active metabolite that was seen with AMG 487. In addition, these compounds also feature increased potency and good pharmacokinetic properties. We will also discuss the efficacy of the lead compound 34 in a mouse model of cellular recruitment induced by bleomycin.Entities:
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Year: 2009 PMID： 19632842 DOI： 10.1016/j.bmcl.2009.07.032
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823