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

作者信息

Cimetière B, Dubuffet T, Landras C, Descombes J J, Simonet S, Verbeuren T J, Lavielle G

机构信息

Institut de Recherches Servier, Centre de Recherches de Croissy, Croissy-sur-Seine, France.

出版信息

Bioorg Med Chem Lett. 1998 Jun 2;8(11):1381-6. doi: 10.1016/s0960-894x(98)00221-2.

DOI:10.1016/s0960-894x(98)00221-2
PMID:9871770
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.

摘要

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