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Benzofuran-substituted urea derivatives as novel P2Y1 receptor antagonists
Authors:Reema K Thalji  Nambi Aiyar  Elizabeth A Davenport  Joseph A Erhardt  Lorena A Kallal  Dwight M Morrow  Shobha Senadhi  Cynthia L Burns-Kurtis  Joseph P Marino
Institution:1. Department of Chemistry, Infectious Diseases Centre for Excellence in Drug Discovery, GlaxoSmithKline, 1250 South Collegeville Road, Collegeville, PA 19426, USA;2. Department of Biology, Metabolic Pathways Centre for Excellence in Drug Discovery, GlaxoSmithKline, 709 Swedeland Road, King of Prussia, PA 19406, USA;3. Department of Biological Reagents and Assay Development, GlaxoSmithKline, 1250 South Collegeville Road, Collegeville, PA 19426, USA;4. Cancer Research, GlaxoSmithKline, 1250 South Collegeville Road, Collegeville, PA 19426, USA;5. Stem Cell Discovery Performance Unit, GlaxoSmithKline, 1250 South Collegeville Road, Collegeville, PA 19426, USA;6. Department of Chemistry, Metabolic Pathways Centre for Excellence in Drug Discovery, GlaxoSmithKline, 709 Swedeland Road, King of Prussia, PA 19406, USA
Abstract:Benzofuran-substituted urea analogs have been identified as novel P2Y1 receptor antagonists. Structure–activity relationship studies around the urea and the benzofuran moieties resulted in compounds having improved potency. Several analogs were shown to inhibit ADP-mediated platelet activation.
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