Optimization of the heterocyclic core of the quinazolinone-derived CXCR3 antagonists
| Autor: | Jason Duquette, Lawrence R. McGee, Xiaohui Du, Tim Sullivan, Julio C. Medina, Jay Danao, George Tonn, Michael G. Johnson, Darin J. Gustin, Zice Fu, Jeffrey Deignan, Ji Ma, Liusheng Zhu, Liang Tang, Andrew P. Marcus, An-Rong Li, Phillipe Bergeron, Xiaoqi Chen, Bryan Lemon, Jiwen Liu, Tassie L. Collins, Teresa Arazas Carabeo, Jeffrey T. Mihalic |
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| Rok vydání: | 2008 |
| Předmět: |
Receptors
CXCR3 medicine.drug_class Stereochemistry Clinical Biochemistry Pharmaceutical Science Carboxamide Biochemistry Chemical synthesis Sulfone chemistry.chemical_compound Heterocyclic Compounds In vivo Drug Discovery Pyrazolopyridine medicine Animals Humans Molecular Biology Quinazolinone Chromatography High Pressure Liquid Quinazolinones Bicyclic molecule Organic Chemistry Stereoisomerism In vitro Rats chemistry Molecular Medicine |
| Zdroj: | Bioorganic & Medicinal Chemistry Letters. 18:688-693 |
| ISSN: | 0960-894X |
| DOI: | 10.1016/j.bmcl.2007.11.060 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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