Dihydropyrimidinones--a new class of anti-staphylococcal antibiotics

Bioorg Med Chem Lett. 2003 Jan 20;13(2):241-5. doi: 10.1016/s0960-894x(02)00880-6.

Abstract

We report the synthesis and pharmacological evaluation of new derivatives of natural dipeptide antibiotic TAN-1057 A, B. In the course of this program, we identified novel analogues of the natural product that display similar antibacterial activity and showed improved tolerability.

MeSH terms

  • Anti-Bacterial Agents / chemical synthesis*
  • Anti-Bacterial Agents / pharmacology*
  • Antineoplastic Agents / chemical synthesis
  • Antineoplastic Agents / pharmacology
  • Dipeptides / chemical synthesis
  • Dipeptides / chemistry
  • Dipeptides / pharmacology
  • Drug Screening Assays, Antitumor
  • Humans
  • Macrophages / drug effects
  • Macrophages / metabolism
  • Microbial Sensitivity Tests
  • Protein Synthesis Inhibitors / chemical synthesis
  • Protein Synthesis Inhibitors / pharmacology
  • Pyrimidinones / chemical synthesis*
  • Pyrimidinones / pharmacology*
  • Staphylococcus / drug effects*
  • Structure-Activity Relationship
  • Tumor Cells, Cultured

Substances

  • Anti-Bacterial Agents
  • Antineoplastic Agents
  • Dipeptides
  • Protein Synthesis Inhibitors
  • Pyrimidinones
  • TAN 1057A