Combinatorial synthesis of anilinoanthraquinone derivatives and evaluation as non-nucleotide-derived P2Y 2 receptor antagonists

…, P Hillmann, M Kaulich, AM Hunder, IA Müller…

Index: Weyler, Stefanie; Baqi, Younis; Hillmann, Petra; Kaulich, Marko; Hunder, Andrea M.; Mueller, Ingrid A.; Mueller, Christa E. Bioorganic and Medicinal Chemistry Letters, 2008 , vol. 18, # 1 p. 223 - 227

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Citation Number: 43

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 ...