Potent and selective thrombin inhibitors featuring hydrophobic, basic P3-P4-aminoalkyllactam moieties

Bioorg Med Chem Lett. 1998 Dec 15;8(24):3525-30. doi: 10.1016/s0960-894x(98)00636-2.

Abstract

Crystal structure and evolving SAR considerations of potent, selective benzylsulfonamide lactam thrombin inhibitors and related serine protease inhibitors have led to the design of novel thrombin inhibitors 1a-g, featuring hydrophobic, basic, P4-alkylaminolactam scaffolds that serve as novel types of P3-P4 dipeptide mimics. The design, synthesis, and biological activity of these targets is presented.

MeSH terms

  • Antithrombins / chemistry*
  • Antithrombins / pharmacology
  • Lactones / chemistry*
  • Structure-Activity Relationship

Substances

  • Antithrombins
  • Lactones