6-Acylamino-penam derivatives: synthesis and inhibition of cathepsins B, L, K, and S

Bioorg Med Chem Lett. 2002 Dec 2;12(23):3417-9. doi: 10.1016/s0960-894x(02)00766-7.

Abstract

The synthesis of a new series of 6-acylamino penam derivatives and their inhibition of cysteine proteases cathepsins B, L, K, and S is described. The 6-acylamino-penam sulfone compounds showed excellent cathepsin L, K, and S inhibition activity with IC(50) values in the nanomolar and subnanomolar range.

MeSH terms

  • Amines / chemistry*
  • Cathepsins / antagonists & inhibitors*
  • Cysteine Proteinase Inhibitors / chemical synthesis*
  • Cysteine Proteinase Inhibitors / pharmacology*
  • Inhibitory Concentration 50
  • Lactams / chemistry*
  • Lactams / pharmacology*
  • Structure-Activity Relationship
  • Sulfones / chemistry*
  • Sulfones / pharmacology*

Substances

  • Amines
  • Cysteine Proteinase Inhibitors
  • Lactams
  • Sulfones
  • 4-oxa-1-azabicyclo(3.2.0)heptan-7-one
  • Cathepsins