Thrombin inhibitors based on [5,5] trans-fused indane lactams

Bioorg Med Chem Lett. 1999 Jun 21;9(12):1657-62. doi: 10.1016/s0960-894x(99)00244-9.

Abstract

A series of trans-fused lactams containing the indane nucleus has been prepared. Compound 19 has much enhanced plasma stability compared with its lactone counterpart and shows appreciable in vitro anticoagulant activity.

MeSH terms

  • Anticoagulants / chemical synthesis
  • Anticoagulants / pharmacology*
  • Binding Sites
  • Enzyme Inhibitors / chemical synthesis
  • Enzyme Inhibitors / pharmacology
  • Indans / chemical synthesis
  • Indans / pharmacology*
  • Inhibitory Concentration 50
  • Lactams / chemical synthesis
  • Lactams / pharmacology*
  • Models, Molecular
  • Structure-Activity Relationship
  • Thrombin / antagonists & inhibitors*

Substances

  • Anticoagulants
  • Enzyme Inhibitors
  • Indans
  • Lactams
  • Thrombin