Improved synthesis of substituted 2-aryl-n-[2-(dimethylamino)ethyl] quinolin-4-amines and their activity as antagonists of immunostimulatory CpG-oligodeoxynucleotides

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Abstract

A general methodology for the synthesis of substituted quinolin-4-amines developed by us previously has been simplified. The synthesized compounds, depending on substituents, show activities in the range from 35 nM to 550 nM as antagonists of immunostimulatory oligodeoxynucleotides containing a CpG motif. A SAR analysis is presented.

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Paliakov, E., Henary, M., Say, M., Janda, L., Manzel, L., Macfarlane, D. E., & Strekowski, L. (2007). Improved synthesis of substituted 2-aryl-n-[2-(dimethylamino)ethyl] quinolin-4-amines and their activity as antagonists of immunostimulatory CpG-oligodeoxynucleotides. Heterocyclic Communications, 13(1), 9–12. https://doi.org/10.1515/HC.2007.13.1.9

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