Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1375561 | Bioorganic & Medicinal Chemistry Letters | 2009 | 6 Pages |
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 IC50 of 2.16 μM. 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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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Erwan Ayral, Philippe Gloanec, Gilbert Bergé, Guillaume de Nanteuil, Philippe Mennecier, Alain Rupin, Tony J. Verbeuren, Pierre Fulcrand, Jean Martinez, Jean-François Hernandez,