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Updated: Jun 26, 2026

Flow Cytometry Analysis of Tissue Factor Expression in Human Platelets
Published on: November 22, 2024
Design, synthesis, and biological evaluation of 1,5-benzothiazepine-4-one derivatives targeting factor VIIa/tissue
Erwan Ayral1, Philippe Gloanec, Gilbert Bergé
1Institut des Biomolécules Max Mousseron, CNRS UMR5247, Université Montpellier 1, Université Montpellier 2, Faculté de Pharmacie, 15 Avenue Charles Flahault, 34093 Montpellier Cedex 5, France.
Abstract:
The 1,5-benzothiazepine-4-one scaffold was earlier shown to provide efficient protease inhibitors. In this contribution, we describe its use in the design of factor VIIa/tissue factor inhibitors. A series containing a scaffold non-substituted on its aryl part led to compound 20 with an IC(50) of 2.16 microM. Following molecular modelling studies of this compound, a second series was prepared, which necessitated the synthesis of protected 7- or 8-substituted 1,5-benzothiazepine-4-one derivatives.
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