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Bioorg Med Chem Lett. 2009 Sep 1;19(17):5114-8. doi: 10.1016/j.bmcl.2009.07.032. Epub 2009 Jul 10.

Optimization of a series of quinazolinone-derived antagonists of CXCR3.

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Amgen Inc., 1120 Veterans Boulevard, South San Francisco, CA 94080, USA.


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.

[Indexed for MEDLINE]

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