Optimization of the heterocyclic core of the quinazolinone-derived CXCR3 antagonists
AR Li, MG Johnson, J Liu, X Chen, X Du… - Bioorganic & medicinal …, 2008 - Elsevier
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.
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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