Ketene aminal-based lactam derivatives as a novel class of orally active FXa inhibitors

Bioorg Med Chem Lett. 2005 Dec 15;15(24):5453-8. doi: 10.1016/j.bmcl.2005.08.107. Epub 2005 Oct 5.

Abstract

N,N'-Disubstituted ketene aminals are good bioisosteres of thiourea functional groups. We report the design and synthesis of a novel class of ketene aminal-based lactam derivatives as potent and orally active FXa inhibitors.

MeSH terms

  • Administration, Oral
  • Ethylenes / administration & dosage
  • Ethylenes / chemistry
  • Ethylenes / pharmacology*
  • Factor Xa Inhibitors*
  • Humans
  • Ketones / administration & dosage
  • Ketones / chemistry
  • Ketones / pharmacology*
  • Lactams / administration & dosage
  • Lactams / pharmacology*
  • Models, Molecular
  • Molecular Conformation
  • Structure-Activity Relationship

Substances

  • Ethylenes
  • Factor Xa Inhibitors
  • Ketones
  • Lactams
  • ketene