Article ID Journal Published Year Pages File Type
1365394 Bioorganic & Medicinal Chemistry Letters 2008 6 Pages PDF
Abstract

A series of six–six and six–five fused heterocyclic CXCR3 antagonists has been synthesized and their activities evaluated in an [125I]-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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Physical Sciences and Engineering Chemistry Organic Chemistry
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