Novel benzo-fused lactam scaffolds as factor Xa inhibitors

S Y Tamura; E A Goldman; P W Bergum; J E Semple

doi:10.1016/s0960-894x(99)00417-5

Novel benzo-fused lactam scaffolds as factor Xa inhibitors

Bioorg Med Chem Lett. 1999 Sep 6;9(17):2573-8. doi: 10.1016/s0960-894x(99)00417-5.

Authors

S Y Tamura¹, E A Goldman, P W Bergum, J E Semple

Affiliation

¹ Corvas International, Inc., Department of Medicinal Chemistry, San Diego, California 92121, USA.

PMID: 10498211
DOI: 10.1016/s0960-894x(99)00417-5

Abstract

Rigid benzolactam P3-P2 dipeptide mimics were designed and prepared as potential inhibitors of blood coagulation factor Xa. Methoxy substitution of the tetrahydrobenzazepinone scaffold led to potent and selective inhibitors. The synthesis and biological activities of these derivatives are reported herein.

MeSH terms

Drug Design
Factor Xa Inhibitors*
Lactams / chemical synthesis
Lactams / chemistry
Lactams / pharmacology*
Serine Proteinase Inhibitors / chemical synthesis
Serine Proteinase Inhibitors / chemistry
Serine Proteinase Inhibitors / pharmacology*

Substances

Factor Xa Inhibitors
Lactams
Serine Proteinase Inhibitors