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Article Dans Une Revue Bioorganic and Medicinal Chemistry Letters Année : 2009

Design, synthesis, and biological evaluation of 1,5-benzothiazepine-4-one derivatives targeting factor VIIa/tissue factor

E. Ayral
  • Fonction : Auteur
P. Gloanec
  • Fonction : Auteur
G. Nanteuil
  • Fonction : Auteur
P. Mennecier
  • Fonction : Auteur
A. Rupin
  • Fonction : Auteur
T. J. Verbeuren
  • Fonction : Auteur

Résumé

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 mu M. 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. (C) 2009 Elsevier Ltd. All rights reserved.

Dates et versions

hal-00389293 , version 1 (28-05-2009)

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Citer

E. Ayral, P. Gloanec, Gilbert Berge, G. Nanteuil, P. Mennecier, et al.. Design, synthesis, and biological evaluation of 1,5-benzothiazepine-4-one derivatives targeting factor VIIa/tissue factor. Bioorganic and Medicinal Chemistry Letters, 2009, 19 (5), pp.1386-1391. ⟨10.1016/j.bmcl.2009.01.039⟩. ⟨hal-00389293⟩
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