Abstract
A library of anilinoanthraquinone derivatives was synthesized by parallel Ullmann coupling reaction of bromaminic acid with aniline derivatives in solution using a compact parallel synthesizer. The products were purified by HPLC and evaluated as antagonists at mouse and human P2Y2 receptors. 4-Phenylamino-substituted 1-amino-2-sulfoanthraquinones, for example, 1-amino-4-(2-methoxyphenyl)-2-sulfoanthraquinone (PSB-716), were potent P2Y2 antagonists with IC50 values in the low micromolar range.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Aniline Compounds / chemical synthesis*
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Aniline Compounds / pharmacology*
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Animals
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Anthraquinones / chemical synthesis*
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Anthraquinones / pharmacology*
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Combinatorial Chemistry Techniques
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Humans
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Inhibitory Concentration 50
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Kinetics
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Mice
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Purinergic P2 Receptor Antagonists*
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Receptors, Purinergic P2Y2
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Structure-Activity Relationship
Substances
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Aniline Compounds
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Anthraquinones
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P2RY2 protein, human
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P2ry2 protein, mouse
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Purinergic P2 Receptor Antagonists
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Receptors, Purinergic P2Y2