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New tetrahydronaphthalene derivatives as combined thromboxane receptor antagonists and thromboxane synthase
B Cimetière1, T Dubuffet, C Landras
1Institut de Recherches Servier, Centre de Recherches de Croissy, Croissy-sur-Seine, France.
Bioorganic & Medicinal Chemistry Letters
|January 1, 1999
Abstract:
A pyridine group was linked to the tetrahydronaphthalene moiety of the derivatives described in the preceding paper, to afford new combined thromboxane receptor (TP-receptor) antagonists and synthase inhibitors. The most interesting compound 2f inhibits TXA2 synthase with an IC50 value of 0.64 microM and the aggregation of human platelets with an IC50 value of 0.063 microM and shows a long duration of action in different species after oral administration.