New tetrahydronaphthalene derivatives as combined thromboxane receptor antagonists and thromboxane synthase inhibitors

Article abstract of DOI:10.1016/S0960-894X(98)00221-2

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 μM and the aggregation of human platelets with an IC50 value of 0.063 μM and shows a long duration of action in different species after oral administration.